Calcium Channel

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Calcium Channel製品

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S1573 Fasudil HCl Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Sci China Life Sci, 2024, 67(8):1549-1562
Ren Fail, 2024, 46(2):2396455
PeerJ, 2023, 11:e15494
S1811 Amiloride HCl Amiloride HCl is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).
J Extracell Vesicles, 2024, 13(4):e12426
J Extracell Vesicles, 2024, 13(4):e12426
Virus Res, 2024, 339:199258
S4202 Verapamil HCl Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.
NPJ Precis Oncol, 2024, 8(1):94
Int J Mol Sci, 2024, 25(18)10162
Biomedicines, 2024, 12(4)904
S1808 Nifedipine Nifedipine is a dihydropyridine calcium channel blocker, used to lower hypertension and to treat angina.
Laryngoscope Investig Otolaryngol, 2023, 8(5):1390-1400
Oncogene, 2021, 40(6):1128-1146
Cell Discov, 2020, 6(1):96
S2721 Nilvadipine Nilvadipine (ARC029, FR34235,FK235) is a potent calcium channel blocker with an IC50 of 0.03 nM.
Nat Commun, 2022, 13-1:6117
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2030 Flunarizine 2HCl Flunarizine 2HCl (KW-3149, R14950) is a dihydrochloride salt form which is a calcium channel blocker with a Ki of 68 nM.
Sci Adv, 2023, 9(15):eadf2695
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1905 Amlodipine Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
Cancer Med, 2024, 13(11):e7291
Acta Pharm Sin B, 2023, 13(10):4217-4233
Acta Pharm Sin B, 2023, 13(10):4217-4233
S6657 2-APB (2-Aminoethyl Diphenylborinate) 2-APB (2-Aminoethyl Diphenylborinate) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations.
iScience, 2024, 27(8):110507
Mol Med Rep, 2024, 30(6)220
PLoS Pathog, 2023, 19(3):e1011295
S1293 Cilnidipine Cilnidipine is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment.
Cell Discov, 2020, 6(1):96
Cell Rep, 2020, 32(2):107897
ACS Infect Dis, 2020, acsinfecdis.0c00486
S1748 Nisoldipine Nisoldipine (Sular, BAY K 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.
Biomed Pharmacother, 2022, 145:112432
iScience, 2022, 25(10):105068
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
S1356 Levetiracetam (UCB-L059) Levetiracetam (UCB-L059, SIB-S1) is an anticonvulsant medication used to treat epilepsy. Levetiracetam (UCB-L059, SIB-S1) is an agonist of muscarinic acetylcholine receptors (mAChR). Levetiracetam modulates the presynaptic P/Q-type voltage-dependent calcium (Ca2+) channel.
Front Neurosci, 2023, 17:1336026
bioRxiv, 2023, 2023.11.10.566574
Alzheimers Dement (N Y), 2022, 8(1):e12329
S8380 YM-58483 (BTP2) YM-58483/BTP2 is a blocker of store-operated Ca2+ entry (SOCE), which regulates the activation of non-excitable cells such as lymphocytes.
Cell Death Discov, 2023, 9(1):100
Dev Cell, 2022, S1534-5807(21)01035-2
J Innate Immun, 2022, 1-13
S7924 Bay K 8644 Bay K 8644 is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM.
ACS Nano, 2021, 10.1021/acsnano.1c03517
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09615-y
Journal of Advanced Research, 2020, 10.1016/j.jare.2020.10.005
S3809 Imperatorin Imperatorin (Ammidin, Marmelosin, Pentosalen, 8-Isoamylenoxypsoralen), a naturally occurring psoralen-type furanocoumarin, is a potent myorelaxant agent and acts as a calcium antagonist on vascular smooth muscle.
Pharmaceuticals (Basel), 2023, 10.3390/ph16111595
Metabolites, 2022, 13(1)3
Adv Sci (Weinh), 2020, 7(16):2000925
S1662 Isradipine Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure.
J Cell Sci, 2022, 135(14)jcs260249
Environ Toxicol Chem, 2021, 10.1002/etc.5018
Cell Discov, 2020, 6(1):96
S2114 Dronedarone HCl Dronedarone HCl (SR33589) is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).
Cancers (Basel), 2022, 14(19)4883
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
Cell Syst, 2019, 8(2):97-108
S5478 Dantrolene sodium Dantrolene sodium(F 440) acts as a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors.
PLoS Pathog, 2023, 19(3):e1011295
Transl Stroke Res, 2022, 10.1007/s12975-022-01021-8
Oxid Med Cell Longev, 2021, 2021:8810698
S1813 Amlodipine Besylate Amlodipine Besylate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
Front Pharmacol, 2022, 13:902305
Cell Discov, 2020, 6(1):96
Oncogene, 2019, 38(1):120-139
S1425 Ranolazine 2HCl Ranolazine 2HCl (RS-43285,RS 43285-193,Ranexa, renolazine,Ranolazine dihydrochloride) is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina.
Basic Clin Pharmacol Toxicol, 2023, 133(2):194-201
Cell Rep, 2022, 41(1):111445
Front Pharmacol, 2019, 10:1367
S2482 Manidipine 2HCl Manidipine 2HCl (CV-4093) is a HCl salt form of Manidipine, which is a calcium channel blocker with IC50 of 2.6 nM, used clinically as an antihypertensive. Phase 4.
Adv Sci (Weinh), 2023, 10(11):e2205500
Front Microbiol, 2023, 14:1177391
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S1885 Felodipine Felodipine (CGH-869) is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM.
Bioact Mater, 2022, 14:272-289
Cell Discov, 2020, 6(1):96
ACS Infect Dis, 2020, acsinfecdis.0c00486
S1747 Nimodipine Nimodipine (BAY E 9736) is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure.
Eye Vis (Lond), 2024, 11(1):37
Cell Discov, 2020, 6(1):96
G3 (Bethesda), 2020, 4;10(5):1585-1597
S2017 Benidipine HCl Benidipine HCl (KW-3049,(±)- Benidipine) is a hydrochloride salt form of benidipine which is a dihydropyridine calcium channel blocker.
Cell Discov, 2020, 6(1):96
ACS Infect Dis, 2020, acsinfecdis.0c00486
Life Sci, 2019, 227:74-81
S3931 Ginsenoside Rd Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Drug Des Devel Ther, 2022, 16:2767-2782
J Ginseng Res, 2022, 46(5):700-709
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S2415 Astragaloside A Astragaloside A (Astragaloside IV) is the primary pure saponin isolated from Astragalus membranaceus, which has been widely used for the treatment of cardiovascular diseases.
Sci Rep, 2022, 12(1):7
Carcinogenesis, 2020, 41(7):993-1004
J Med Virol, 2019, 91(8):1440-1447
S1799 Ranolazine Ranolazine (CVT 303, RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina.
Sci Rep, 2023, 10.1038/s41598-023-47540-8
Cancer Cell, 2022, S1535-6108(22)00312-9
S2535 Econazole nitrate Econazole Nitrate (NSC 243115,Spectazole) is a Ca2+ channel blocker, used as an antifungal medicine that fights infections caused by fungus.
Nat Commun, 2024, 15(1):8708
Cell Rep Med, 2023, 4(12):101309
Int J Mol Sci, 2022, 23(22)13809
S4181 Nicardipine HCl Nicardipine HCl (RS-69216,YC-93) is a dihydropyridine calcium-channel blocking agent used for the treatment of vascular disorders.
Cell Discov, 2020, 6(1):96
ACS Infect Dis, 2020, acsinfecdis.0c00486
S3053 Azelnidipine Azelnidipine (UR-12592) is a dihydropyridine calcium channel blocker.
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S1865 Diltiazem HCl Diltiazem (Tiazac, RG 83606) HCl is a benzothiazepine derivative with vasodilating action due to its antagonism of the actions of the calcium ion in membrane functions.
J Cell Mol Med, 2018, 22(12):5964-5977
FASEB J, 2017, 31(2):625-635
S2397 Palmatine chloride Palmatine hydrochloride (Palmatine chloride (6CI,7CI); Fibrauretin) is a hydrochloride salt of palmatine which is a protoberberine alkaloid.
Molecules, 2021, 26(5)1210
J Med Virol, 2019, 91(8):1440-1447
S4648 Dantrolene sodium hemiheptahydrate Dantrolene sodium hemiheptahydrate (Dantrium) is a skeletal muscle relaxant that acts by interfering with excitation-contraction coupling in the muscle fiber.
Cardiovasc Res, 2021, 117(4):1091-1102
Oxid Med Cell Longev, 2021, 2021:8810698
S6847 ML-9 HCl ML-9 HCl (ML-9 hydrochloride) is a selective and potent inhibitor of Akt kinase, myosin light chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). ML-9 HCl is also a potent inhibitor of Ca2+-permeable channels. ML-9 HCl is a lysosomotropic agent targeting autophagy and cell death.
PLoS Pathog, 2023, 19(3):e1011295
J Mol Endocrinol, 2019, 63(3):199-213
S2481 Manidipine Manidipine(CV-4093,(±)-Manidipine) is a calcium channel blocker (dihydropyridine type) that is used clinically as an antihypertensive.
Antiviral Res, 2018, 150:130-136
S2446 Levosimendan Levosimendan(OR1259,OR1855,Simsndan) is a calcium sensitizer acting through calcium-dependent binding to cardiac troponin C (cTnC), provides treatment for heart failure.
Antiviral Res, 2017, 146:76-85
S2080 Clevidipine Butyrate Clevidipine Butyrate(Cleviprex) is a dihydropyridine calcium channel blocker, uses as an agent for the reduction of blood pressure.
ACS Infect Dis, 2020, acsinfecdis.0c00486
S2573 Tetracaine HCl Tetracaine HCl (Amethocaine hydrochloride) is a hydrochloride salt form of tetracaine which is a potent local anaesthetic and a channel function allosteric inhibitor.
PLoS Pathog, 2023, 19(3):e1011295
S5255 Nicardipine Nicardipine is a potent calcium channel blockader with marked vasodilator action.
Cell Chem Biol, 2021, S2451-9456(21)00442-6
S4626 Ethosuximide Ethosuximide(Zarontin) is a succinimide anticonvulsant, used mainly in absence seizures; A calcium channel blocker.
Nature, 2018, 554(7692):317-322
S5966 Amlodipine maleate Amlodipine (Amvaz, UK-48340) maleate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
Front Pharmacol, 2022, 13:902305
S4597 Lercanidipine hydrochloride Lercanidipine is a calcium channel blocker of the dihydropyridine class.
J Phys Chem B, 2013, 117(23):6868-73
S4977 Efonidipine Efonidipine (NZ-105) is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. It also suppresses aldosterone secretion from the adrenal.
Biomol Ther (Seoul), 2022, 30(5):455-464
S5191 Cinacalcet Cinacalcet (AMG073, Sensipar, Cin) is an orally active, allosteric agonist of receptors for calcium (CaR) that increases the sensitivity of the CaR to Ca.
Int J Mol Sci, 2022, 23(8)4323
S6834 Zegocractin (CM 4620) Zegocractin (CM 4620) is an inhibitor of calcium-release activated calcium-channel (CRAC channel). CM4620 inhibits Orai1/STIM1-mediated Ca2+ currents and Orai2/STIM1-mediated currents with IC50 of near 120 nM and 900 nM, respectively.
Elife, 2023, 12e81288
S5514 Lanthanum(III) chloride heptahydrate Lanthanum(III) chloride is the inorganic compound used in biochemical research to block the activity of divalent cation channels, mainly calcium channels.
J Surg Res, 2021, 263:236-244
S3766 Tanshinone IIA sulfonate sodium Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
J Inflamm Res, 2022, 15:6293-6306
S3674 Levamlodipine Levamlodipine (S-amlodipine) is a pharmacologically active enantiomer of amlodipine which belongs to the dihydropyridine group of calcium channel blocker. It acts on the L-type of calcium channels and its treatment results in vasodilation and a fall in blood pressure.
Oncogene, 2021, 40(6):1128-1146
S7074 Ionomycin Ionomycin (SQ23377) is a potent and selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. It induces the activation of protein kinase C (PKC) and promotes apoptosis.
Diabetes, 2024, db231000
Am J Physiol Cell Physiol, 2020, 10.1152/ajpcell.00290.2020
S4727 Cinnarizine Cinnarizine (Stugeron, Dimitronal, Stutgin, Cinarizine) is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker.
Sci Adv, 2022, 8(15):eabk2376
S1994 Lacidipine Lacidipine (GX-1048, GR-43659X, SN-305) is a L-type calcium channel blocker, used for treating high blood pressure.
S2491 Nitrendipine Nitrendipine (Bayotensin) is a dihydropyridine calcium channel blocker with an IC50 of 95 nM.
Nat Commun, 2024, 15(1):8708
S2050 Strontium Ranelate Strontium Ranelate is a strontium(II) salt of ranelic acid for (-)-desmethoxyverapamil binding to calcium channel with IC50 of 0.5 mM.
S1911 Disodium Cromoglycate Disodium Cromoglycate (Gynazole ,FPL 670 (Cromolyn) Disodium,Cromolyn sodium) is an antiallergic drug with IC50 of 39 μg/mL.
S0000 Cav 2.2 blocker 1 Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 0.001 μM.
S0713 S107 hydrochloride S107 hydrochloride is a specific stabilizer of RyR2 (type 2 ryanodine receptor)/FKBP12.6 (FK506 binding protein 12.6) complex that affects Ca2+ signaling.
E0778 o-3M3FBS O-3M3FBS, the negative control of m-3M3FBS, inhibits inward and outward currents via mechanisms independent of PLC acting in an antagonistic manner, reversibly inhibits delayed rectifier K+ channels, increases in [Ca2+](i) in an agonistic manner with m-3M3FBS.
S3236 Mesaconitine Mesaconitine, one of the aconite alkaloids in Aconiti tuber, increases the [Ca2+]i level in endothelial cells by influx of Ca2+ from extracellular spaces.
S6994 TD-165 TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group.
E4039 (S)-(-)-Bay K8644 (S)-(-)-Bay K8644, a conventional racemic mixture of Bay K 8644, is a voltage-sensitive L-type calcium channel agonist. It also activates Ba2+ currents (Iba) with EC50 of 32 nM.
S4931 Propiverine hydrochloride Propiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence.
S3045 Cinepazide maleate Cinepazide maleate is a maleate salt form of cinepazide which is a vasodilator.
S3242 Loureirin B Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular.
S0535 FK962 FK962, a derivative of FK960 with putative anti-dementia properties, significantly enhances high K+-evoked somatostatin release from rat hippocampal slices at 1-1000 nM, also significantly reduces somatostatin-induced inhibition of Ca2+ channels at 1-100 nM in single rat hippocampal neurons.
S0870 Barnidipine Barnidipine (Libradin, Mepirodipine, Vasexten, YM-09730-5, Cyress, Hypoca, Oldeca) is an antihypertensive drug that belongs to the dihydropyridine (DHP) group of calcium antagonist (CaA) with Ki of 0.21 nM for [3H]nitrendipine binding sites.
S0973 Wilforgine Wilforgine, one of the major bioactive sesquiterpene alkaloids in Tripterygium wilfordii Hook. F., induces microstructural and ultrastructural changes in the muscles of M. separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system.
E4919New Barnidipine hydrochloride Barnidipine hydrochloride(Mepirodipine hydrochloride, YM-09730-5) is an antagonist of L-type calcium (CaA). It displays a high affinity for [3H] initrendipine binding sites with a Ki value of 0.21 nmol/l. Barnidipine hydrochloride also acts as an antihypertensive agent.
S5279 Fendiline hydrochloride Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras.
S3845 Panaxadiol Panaxadiol (20(R)-Panaxadiol) is a triterpene sapogenin originally found in species of Panax (ginseng) and exhibits anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities. It inhibits Ca2+ channels, decreasing channel open time and open state probability in vitro and displaying anti-arrhythmic potential.
S5898 Efonidipine hydrochloride monoethanolate Efonidipine (NZ-105) hydrochloride monoethanolate is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. Efonidipine hydrochloride monoethanolate also suppresses aldosterone secretion from the adrenal.
E4980New Verapamil Verapamil(Iproveratril,Dilacoran), is a phenylalkylamine derivative which is an antagonist of calcium influx and also an inhibitor P-gp and CYP3A4. It exhibits potency in treatment for angina, cardiac arrhythmias, cardiomyopathies and hypertension.
S3700 DHBP dibromide DHBP (1,1'-diheptyl-4,4'-bipyridinium), a viologen for electrochromic memory display agent, inhibits the calcium release induced by 2 mM caffeine and 2 μg/ml polylysine with an IC50 value of 5 μg/ml and 4 μg/ml respectively.
E1368 PD173212 PD173212(Compound 11) is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.
E0936 IGS-1.76 IGS-1.76, a protein-protein interaction (PPI) inhibitor, which exerts drug-like properties showing a significantly affinity for human neuronal calcium sensor 1 (hNCS-1), and efficiently modulates the interaction of hNCS-1 and guanine exchange factor Ric8a.
S9017 Columbianadin Columbianadin (Zosimin, 2-Butenoic acid), a natural coumarin from Angelica decursiva, is known to have various biological activities including calcium-channel blocking activity, cytotoxic activity against various cancer cell lines, analgesic activities, intestinal absorption and transportation, anti-inflammatory and anti-cancer effects.
S2403 Tetrandrine Tetrandrine, a bis-benzylisoquinoline alkaloid derived from Stephania tetrandra, is a calcium channel blocker.
Pharmacol Res, 2024, 207:107314
mBio, 2024, e0228723.
Virus Res, 2024, 339:199258
S9315 Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S6920 SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
S4084 Lomerizine 2HCl Lomerizine dihydrochloride (KB-2796) is a relatively new L- and T-type calcium channel blocker used in the treatment of migraine.
Nat Commun, 2024, 15(1):8708
E0826 Levamlodipine Besylate Levamlodipine Besylate is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
E0945 BIA BIA (TMBIM6 antagonist BIA), a potential TMBIM6 antagonist, is an inhibitor of the interaction between TMBIM6 (Transmembrane B cell lymphoma 2-associated X protein (BAX) inhibitor motif-containing 6) and mTORC2, which ultimately blocks AKT activation and cancer progression.
S3682 Ethyl 3-Aminobenzoate methanesulfonate Ethyl 3-Aminobenzoate (Ethyl m-Aminobenzoate, NSC 93790, Tricaine) can block the generation of action potentials via voltage-dependent Na+-channels and usually used for anesthesia, sedation, or euthanasia of fish.
E0334 BAMB-4 BAMB-4 (ITPKA-IN-C14) is a new type of membrane permeable ITPKA inhibitor, and IC50 is 37 μM in the Kinase ADP-Glo assay.
S9400 Rhynchophylline Rhynchophylline (Mitrinermine), an active component isolated from species of the genus Uncaria, acts as a calcium channel blocker and is widely used in traditional Chinese medicine mainly for treating ailments of central nervous and cardiovascular systems, such as lightheadedness, convulsions, numbness, and hypertension.
E0777 Z944 Z944 is a highly selective antagonist for T-type calcium channel with IC50s of 50, 160, 110 nM for hCaV3.1, hCaV3.2, and hCaV3.3.
S3883 Protopine Protopine (Corydinine, Fumarine, Biflorine, Macleyine), an alkaloid present in different plants, has been shown to exhibit a number of activities, such as inhibition of calcium influx through both voltage and receptor-operated channels and inhibition of rabbit blood platelet aggregation. It also possesses anti-cholinergic and anti-histaminic as well as anti-bacterial activities.
S3191 Azumolene Azumolene (EU4093 free base), an equipotent dantrolene analog, is a ryanodine receptor (RyR) modulator that inhibits the calcium-release.
S5567 Trimethadione Trimethadione is an oxazolidinedione anticonvulsant and often used to treat epileptic conditions that are resistant to other treatments.
S4353 Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
S9566 Bepridil hydrochloride Bepridil hydrochloride(CERM 1978) is an anti-anginal drug classified as a calcium channel blocker. It also blocks multiple other ion channels, including sodium and potassium channels.
S2436 Pranidipine Pranidipine (Acalas, OPC 13340) is a new 1,4-dihydropyridine calcium channel blocker. Pranidipine can enhance cyclic GMP-independent nitric oxide-induced relaxation of the rat aorta.
S0452 NP118809 NP118809(39-1B4) is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM, also less potently inhibits L-type calcium channel with an IC50 of 12.2 μM.
E2691 BAPTA tetrapotassium salt BAPTA tetrapotassium salt (BAPTA tetrapotassium) is a non-permeable, selective extracellular calcium chelator, with 105-fold greater affinity for Ca2+ than Mg2+, which is a valuable tool to study the role of calcium in cell signaling.
S0016 SN-6 SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation.
S9151 Praeruptorin E Praeruptorin E, isolated from Peucedanum praeruptorum Dunn., is a cardiotonic agent with selective cardiac calcium channel agonistic effect.
S6473 Pinaverium bromide Pinaverium bromide (Icosapentaenoic acid) acts as a calcium channel blocker and is useful for functional gastrointestinal disorders.
E1410 Fluspirilene Fluspirilene(R 6218; Redeptin) is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM in cell-free assays. Fluspirileneis a long-acting injectable depot antipsychotic agent used for schizophrenia.
E2984 GSK-7975A GSK-7975A is a potent and orally available inhibitor of CRAC channel. It reduces FcεRI-dependent Ca2+ influx and reduces the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα).
E0137 GV-58 GV-58 is a novel, selective N-type and P/Q-type Ca2+ channels agonist with IC50s of 7.21 μM and 8.81 μM, respectively.
S5861 Lercanidipine Lercanidipine is a vasoselective dihydropyridine calcium antagonist used for the treatment of essential hypertension.
S9842 MCU-i4 MCU-i4 is a negative modulator of the mitochondrial calcium uniporter (MCU) complex that directly binds a specific cleft in MICU1 and decreases mitochondrial Ca2+ influx.
E2993 Ruthenium Red Ruthenium red (Ammoniated ruthenium oxychloride) is a polycationic dye, which is a L-type calcium current (ICa) blocker. It is widely used for electron microscopy (EM) of cells, tissues and vegetative bacteria. Ruthenium red strongly reacts with phospholipids and fatty acids and binds to acidic mucopolysaccharides.
S5191 Cinacalcet Cinacalcet (AMG073, Sensipar, Cin) is an orally active, allosteric agonist of receptors for calcium (CaR) that increases the sensitivity of the CaR to Ca.
Int J Mol Sci, 2022, 23(8)4323
E4039 (S)-(-)-Bay K8644 (S)-(-)-Bay K8644, a conventional racemic mixture of Bay K 8644, is a voltage-sensitive L-type calcium channel agonist. It also activates Ba2+ currents (Iba) with EC50 of 32 nM.
S9151 Praeruptorin E Praeruptorin E, isolated from Peucedanum praeruptorum Dunn., is a cardiotonic agent with selective cardiac calcium channel agonistic effect.
E0137 GV-58 GV-58 is a novel, selective N-type and P/Q-type Ca2+ channels agonist with IC50s of 7.21 μM and 8.81 μM, respectively.
S1573 Fasudil HCl Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Sci China Life Sci, 2024, 67(8):1549-1562
Ren Fail, 2024, 46(2):2396455
PeerJ, 2023, 11:e15494
S1811 Amiloride HCl Amiloride HCl is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).
J Extracell Vesicles, 2024, 13(4):e12426
J Extracell Vesicles, 2024, 13(4):e12426
Virus Res, 2024, 339:199258
S4202 Verapamil HCl Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.
NPJ Precis Oncol, 2024, 8(1):94
Int J Mol Sci, 2024, 25(18)10162
Biomedicines, 2024, 12(4)904
S1808 Nifedipine Nifedipine is a dihydropyridine calcium channel blocker, used to lower hypertension and to treat angina.
Laryngoscope Investig Otolaryngol, 2023, 8(5):1390-1400
Oncogene, 2021, 40(6):1128-1146
Cell Discov, 2020, 6(1):96
S2721 Nilvadipine Nilvadipine (ARC029, FR34235,FK235) is a potent calcium channel blocker with an IC50 of 0.03 nM.
Nat Commun, 2022, 13-1:6117
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2030 Flunarizine 2HCl Flunarizine 2HCl (KW-3149, R14950) is a dihydrochloride salt form which is a calcium channel blocker with a Ki of 68 nM.
Sci Adv, 2023, 9(15):eadf2695
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1905 Amlodipine Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
Cancer Med, 2024, 13(11):e7291
Acta Pharm Sin B, 2023, 13(10):4217-4233
Acta Pharm Sin B, 2023, 13(10):4217-4233
S6657 2-APB (2-Aminoethyl Diphenylborinate) 2-APB (2-Aminoethyl Diphenylborinate) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations.
iScience, 2024, 27(8):110507
Mol Med Rep, 2024, 30(6)220
PLoS Pathog, 2023, 19(3):e1011295
S1293 Cilnidipine Cilnidipine is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment.
Cell Discov, 2020, 6(1):96
Cell Rep, 2020, 32(2):107897
ACS Infect Dis, 2020, acsinfecdis.0c00486
S1748 Nisoldipine Nisoldipine (Sular, BAY K 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.
Biomed Pharmacother, 2022, 145:112432
iScience, 2022, 25(10):105068
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
S1356 Levetiracetam (UCB-L059) Levetiracetam (UCB-L059, SIB-S1) is an anticonvulsant medication used to treat epilepsy. Levetiracetam (UCB-L059, SIB-S1) is an agonist of muscarinic acetylcholine receptors (mAChR). Levetiracetam modulates the presynaptic P/Q-type voltage-dependent calcium (Ca2+) channel.
Front Neurosci, 2023, 17:1336026
bioRxiv, 2023, 2023.11.10.566574
Alzheimers Dement (N Y), 2022, 8(1):e12329
S8380 YM-58483 (BTP2) YM-58483/BTP2 is a blocker of store-operated Ca2+ entry (SOCE), which regulates the activation of non-excitable cells such as lymphocytes.
Cell Death Discov, 2023, 9(1):100
Dev Cell, 2022, S1534-5807(21)01035-2
J Innate Immun, 2022, 1-13
S1662 Isradipine Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure.
J Cell Sci, 2022, 135(14)jcs260249
Environ Toxicol Chem, 2021, 10.1002/etc.5018
Cell Discov, 2020, 6(1):96
S2114 Dronedarone HCl Dronedarone HCl (SR33589) is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).
Cancers (Basel), 2022, 14(19)4883
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
Cell Syst, 2019, 8(2):97-108
S1813 Amlodipine Besylate Amlodipine Besylate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
Front Pharmacol, 2022, 13:902305
Cell Discov, 2020, 6(1):96
Oncogene, 2019, 38(1):120-139
S1425 Ranolazine 2HCl Ranolazine 2HCl (RS-43285,RS 43285-193,Ranexa, renolazine,Ranolazine dihydrochloride) is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina.
Basic Clin Pharmacol Toxicol, 2023, 133(2):194-201
Cell Rep, 2022, 41(1):111445
Front Pharmacol, 2019, 10:1367
S2482 Manidipine 2HCl Manidipine 2HCl (CV-4093) is a HCl salt form of Manidipine, which is a calcium channel blocker with IC50 of 2.6 nM, used clinically as an antihypertensive. Phase 4.
Adv Sci (Weinh), 2023, 10(11):e2205500
Front Microbiol, 2023, 14:1177391
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S1885 Felodipine Felodipine (CGH-869) is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM.
Bioact Mater, 2022, 14:272-289
Cell Discov, 2020, 6(1):96
ACS Infect Dis, 2020, acsinfecdis.0c00486
S1747 Nimodipine Nimodipine (BAY E 9736) is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure.
Eye Vis (Lond), 2024, 11(1):37
Cell Discov, 2020, 6(1):96
G3 (Bethesda), 2020, 4;10(5):1585-1597
S2017 Benidipine HCl Benidipine HCl (KW-3049,(±)- Benidipine) is a hydrochloride salt form of benidipine which is a dihydropyridine calcium channel blocker.
Cell Discov, 2020, 6(1):96
ACS Infect Dis, 2020, acsinfecdis.0c00486
Life Sci, 2019, 227:74-81
S3931 Ginsenoside Rd Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Drug Des Devel Ther, 2022, 16:2767-2782
J Ginseng Res, 2022, 46(5):700-709
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S1799 Ranolazine Ranolazine (CVT 303, RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina.
Sci Rep, 2023, 10.1038/s41598-023-47540-8
Cancer Cell, 2022, S1535-6108(22)00312-9
S4181 Nicardipine HCl Nicardipine HCl (RS-69216,YC-93) is a dihydropyridine calcium-channel blocking agent used for the treatment of vascular disorders.
Cell Discov, 2020, 6(1):96
ACS Infect Dis, 2020, acsinfecdis.0c00486
S3053 Azelnidipine Azelnidipine (UR-12592) is a dihydropyridine calcium channel blocker.
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S1865 Diltiazem HCl Diltiazem (Tiazac, RG 83606) HCl is a benzothiazepine derivative with vasodilating action due to its antagonism of the actions of the calcium ion in membrane functions.
J Cell Mol Med, 2018, 22(12):5964-5977
FASEB J, 2017, 31(2):625-635
S4648 Dantrolene sodium hemiheptahydrate Dantrolene sodium hemiheptahydrate (Dantrium) is a skeletal muscle relaxant that acts by interfering with excitation-contraction coupling in the muscle fiber.
Cardiovasc Res, 2021, 117(4):1091-1102
Oxid Med Cell Longev, 2021, 2021:8810698
S6847 ML-9 HCl ML-9 HCl (ML-9 hydrochloride) is a selective and potent inhibitor of Akt kinase, myosin light chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). ML-9 HCl is also a potent inhibitor of Ca2+-permeable channels. ML-9 HCl is a lysosomotropic agent targeting autophagy and cell death.
PLoS Pathog, 2023, 19(3):e1011295
J Mol Endocrinol, 2019, 63(3):199-213
S2481 Manidipine Manidipine(CV-4093,(±)-Manidipine) is a calcium channel blocker (dihydropyridine type) that is used clinically as an antihypertensive.
Antiviral Res, 2018, 150:130-136
S2080 Clevidipine Butyrate Clevidipine Butyrate(Cleviprex) is a dihydropyridine calcium channel blocker, uses as an agent for the reduction of blood pressure.
ACS Infect Dis, 2020, acsinfecdis.0c00486
S2573 Tetracaine HCl Tetracaine HCl (Amethocaine hydrochloride) is a hydrochloride salt form of tetracaine which is a potent local anaesthetic and a channel function allosteric inhibitor.
PLoS Pathog, 2023, 19(3):e1011295
S5255 Nicardipine Nicardipine is a potent calcium channel blockader with marked vasodilator action.
Cell Chem Biol, 2021, S2451-9456(21)00442-6
S4626 Ethosuximide Ethosuximide(Zarontin) is a succinimide anticonvulsant, used mainly in absence seizures; A calcium channel blocker.
Nature, 2018, 554(7692):317-322
S5966 Amlodipine maleate Amlodipine (Amvaz, UK-48340) maleate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
Front Pharmacol, 2022, 13:902305
S4597 Lercanidipine hydrochloride Lercanidipine is a calcium channel blocker of the dihydropyridine class.
J Phys Chem B, 2013, 117(23):6868-73
S4977 Efonidipine Efonidipine (NZ-105) is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. It also suppresses aldosterone secretion from the adrenal.
Biomol Ther (Seoul), 2022, 30(5):455-464
S6834 Zegocractin (CM 4620) Zegocractin (CM 4620) is an inhibitor of calcium-release activated calcium-channel (CRAC channel). CM4620 inhibits Orai1/STIM1-mediated Ca2+ currents and Orai2/STIM1-mediated currents with IC50 of near 120 nM and 900 nM, respectively.
Elife, 2023, 12e81288
S5514 Lanthanum(III) chloride heptahydrate Lanthanum(III) chloride is the inorganic compound used in biochemical research to block the activity of divalent cation channels, mainly calcium channels.
J Surg Res, 2021, 263:236-244
S3766 Tanshinone IIA sulfonate sodium Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
J Inflamm Res, 2022, 15:6293-6306
S3674 Levamlodipine Levamlodipine (S-amlodipine) is a pharmacologically active enantiomer of amlodipine which belongs to the dihydropyridine group of calcium channel blocker. It acts on the L-type of calcium channels and its treatment results in vasodilation and a fall in blood pressure.
Oncogene, 2021, 40(6):1128-1146
S4727 Cinnarizine Cinnarizine (Stugeron, Dimitronal, Stutgin, Cinarizine) is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker.
Sci Adv, 2022, 8(15):eabk2376
S1994 Lacidipine Lacidipine (GX-1048, GR-43659X, SN-305) is a L-type calcium channel blocker, used for treating high blood pressure.
S2491 Nitrendipine Nitrendipine (Bayotensin) is a dihydropyridine calcium channel blocker with an IC50 of 95 nM.
Nat Commun, 2024, 15(1):8708
S0000 Cav 2.2 blocker 1 Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 0.001 μM.
E0778 o-3M3FBS O-3M3FBS, the negative control of m-3M3FBS, inhibits inward and outward currents via mechanisms independent of PLC acting in an antagonistic manner, reversibly inhibits delayed rectifier K+ channels, increases in [Ca2+](i) in an agonistic manner with m-3M3FBS.
S3045 Cinepazide maleate Cinepazide maleate is a maleate salt form of cinepazide which is a vasodilator.
S3242 Loureirin B Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular.
S0535 FK962 FK962, a derivative of FK960 with putative anti-dementia properties, significantly enhances high K+-evoked somatostatin release from rat hippocampal slices at 1-1000 nM, also significantly reduces somatostatin-induced inhibition of Ca2+ channels at 1-100 nM in single rat hippocampal neurons.
S5279 Fendiline hydrochloride Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras.
S3845 Panaxadiol Panaxadiol (20(R)-Panaxadiol) is a triterpene sapogenin originally found in species of Panax (ginseng) and exhibits anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities. It inhibits Ca2+ channels, decreasing channel open time and open state probability in vitro and displaying anti-arrhythmic potential.
S5898 Efonidipine hydrochloride monoethanolate Efonidipine (NZ-105) hydrochloride monoethanolate is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. Efonidipine hydrochloride monoethanolate also suppresses aldosterone secretion from the adrenal.
S3700 DHBP dibromide DHBP (1,1'-diheptyl-4,4'-bipyridinium), a viologen for electrochromic memory display agent, inhibits the calcium release induced by 2 mM caffeine and 2 μg/ml polylysine with an IC50 value of 5 μg/ml and 4 μg/ml respectively.
E1368 PD173212 PD173212(Compound 11) is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.
S9017 Columbianadin Columbianadin (Zosimin, 2-Butenoic acid), a natural coumarin from Angelica decursiva, is known to have various biological activities including calcium-channel blocking activity, cytotoxic activity against various cancer cell lines, analgesic activities, intestinal absorption and transportation, anti-inflammatory and anti-cancer effects.
S2403 Tetrandrine Tetrandrine, a bis-benzylisoquinoline alkaloid derived from Stephania tetrandra, is a calcium channel blocker.
Pharmacol Res, 2024, 207:107314
mBio, 2024, e0228723.
Virus Res, 2024, 339:199258
S9315 Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S6920 SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
S4084 Lomerizine 2HCl Lomerizine dihydrochloride (KB-2796) is a relatively new L- and T-type calcium channel blocker used in the treatment of migraine.
Nat Commun, 2024, 15(1):8708
E0826 Levamlodipine Besylate Levamlodipine Besylate is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
S3682 Ethyl 3-Aminobenzoate methanesulfonate Ethyl 3-Aminobenzoate (Ethyl m-Aminobenzoate, NSC 93790, Tricaine) can block the generation of action potentials via voltage-dependent Na+-channels and usually used for anesthesia, sedation, or euthanasia of fish.
E0334 BAMB-4 BAMB-4 (ITPKA-IN-C14) is a new type of membrane permeable ITPKA inhibitor, and IC50 is 37 μM in the Kinase ADP-Glo assay.
S9400 Rhynchophylline Rhynchophylline (Mitrinermine), an active component isolated from species of the genus Uncaria, acts as a calcium channel blocker and is widely used in traditional Chinese medicine mainly for treating ailments of central nervous and cardiovascular systems, such as lightheadedness, convulsions, numbness, and hypertension.
S3883 Protopine Protopine (Corydinine, Fumarine, Biflorine, Macleyine), an alkaloid present in different plants, has been shown to exhibit a number of activities, such as inhibition of calcium influx through both voltage and receptor-operated channels and inhibition of rabbit blood platelet aggregation. It also possesses anti-cholinergic and anti-histaminic as well as anti-bacterial activities.
S5567 Trimethadione Trimethadione is an oxazolidinedione anticonvulsant and often used to treat epileptic conditions that are resistant to other treatments.
S9566 Bepridil hydrochloride Bepridil hydrochloride(CERM 1978) is an anti-anginal drug classified as a calcium channel blocker. It also blocks multiple other ion channels, including sodium and potassium channels.
S0452 NP118809 NP118809(39-1B4) is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM, also less potently inhibits L-type calcium channel with an IC50 of 12.2 μM.
S0016 SN-6 SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation.
S6473 Pinaverium bromide Pinaverium bromide (Icosapentaenoic acid) acts as a calcium channel blocker and is useful for functional gastrointestinal disorders.
E2984 GSK-7975A GSK-7975A is a potent and orally available inhibitor of CRAC channel. It reduces FcεRI-dependent Ca2+ influx and reduces the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα).
S9842 MCU-i4 MCU-i4 is a negative modulator of the mitochondrial calcium uniporter (MCU) complex that directly binds a specific cleft in MICU1 and decreases mitochondrial Ca2+ influx.
E2993 Ruthenium Red Ruthenium red (Ammoniated ruthenium oxychloride) is a polycationic dye, which is a L-type calcium current (ICa) blocker. It is widely used for electron microscopy (EM) of cells, tissues and vegetative bacteria. Ruthenium red strongly reacts with phospholipids and fatty acids and binds to acidic mucopolysaccharides.
S7924 Bay K 8644 Bay K 8644 is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM.
ACS Nano, 2021, 10.1021/acsnano.1c03517
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09615-y
Journal of Advanced Research, 2020, 10.1016/j.jare.2020.10.005
S2050 Strontium Ranelate Strontium Ranelate is a strontium(II) salt of ranelic acid for (-)-desmethoxyverapamil binding to calcium channel with IC50 of 0.5 mM.
S3809 Imperatorin Imperatorin (Ammidin, Marmelosin, Pentosalen, 8-Isoamylenoxypsoralen), a naturally occurring psoralen-type furanocoumarin, is a potent myorelaxant agent and acts as a calcium antagonist on vascular smooth muscle.
Pharmaceuticals (Basel), 2023, 10.3390/ph16111595
Metabolites, 2022, 13(1)3
Adv Sci (Weinh), 2020, 7(16):2000925
S4931 Propiverine hydrochloride Propiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence.
S0870 Barnidipine Barnidipine (Libradin, Mepirodipine, Vasexten, YM-09730-5, Cyress, Hypoca, Oldeca) is an antihypertensive drug that belongs to the dihydropyridine (DHP) group of calcium antagonist (CaA) with Ki of 0.21 nM for [3H]nitrendipine binding sites.
E4919New Barnidipine hydrochloride Barnidipine hydrochloride(Mepirodipine hydrochloride, YM-09730-5) is an antagonist of L-type calcium (CaA). It displays a high affinity for [3H] initrendipine binding sites with a Ki value of 0.21 nmol/l. Barnidipine hydrochloride also acts as an antihypertensive agent.
E4980New Verapamil Verapamil(Iproveratril,Dilacoran), is a phenylalkylamine derivative which is an antagonist of calcium influx and also an inhibitor P-gp and CYP3A4. It exhibits potency in treatment for angina, cardiac arrhythmias, cardiomyopathies and hypertension.
E0945 BIA BIA (TMBIM6 antagonist BIA), a potential TMBIM6 antagonist, is an inhibitor of the interaction between TMBIM6 (Transmembrane B cell lymphoma 2-associated X protein (BAX) inhibitor motif-containing 6) and mTORC2, which ultimately blocks AKT activation and cancer progression.
E0777 Z944 Z944 is a highly selective antagonist for T-type calcium channel with IC50s of 50, 160, 110 nM for hCaV3.1, hCaV3.2, and hCaV3.3.
S2436 Pranidipine Pranidipine (Acalas, OPC 13340) is a new 1,4-dihydropyridine calcium channel blocker. Pranidipine can enhance cyclic GMP-independent nitric oxide-induced relaxation of the rat aorta.
E1410 Fluspirilene Fluspirilene(R 6218; Redeptin) is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM in cell-free assays. Fluspirileneis a long-acting injectable depot antipsychotic agent used for schizophrenia.
S5861 Lercanidipine Lercanidipine is a vasoselective dihydropyridine calcium antagonist used for the treatment of essential hypertension.
S5191 Cinacalcet Cinacalcet (AMG073, Sensipar, Cin) is an orally active, allosteric agonist of receptors for calcium (CaR) that increases the sensitivity of the CaR to Ca.
Int J Mol Sci, 2022, 23(8)4323
E4039 (S)-(-)-Bay K8644 (S)-(-)-Bay K8644, a conventional racemic mixture of Bay K 8644, is a voltage-sensitive L-type calcium channel agonist. It also activates Ba2+ currents (Iba) with EC50 of 32 nM.
S9151 Praeruptorin E Praeruptorin E, isolated from Peucedanum praeruptorum Dunn., is a cardiotonic agent with selective cardiac calcium channel agonistic effect.
E0137 GV-58 GV-58 is a novel, selective N-type and P/Q-type Ca2+ channels agonist with IC50s of 7.21 μM and 8.81 μM, respectively.
S2415 Astragaloside A Astragaloside A (Astragaloside IV) is the primary pure saponin isolated from Astragalus membranaceus, which has been widely used for the treatment of cardiovascular diseases.
Sci Rep, 2022, 12(1):7
Carcinogenesis, 2020, 41(7):993-1004
J Med Virol, 2019, 91(8):1440-1447
S2535 Econazole nitrate Econazole Nitrate (NSC 243115,Spectazole) is a Ca2+ channel blocker, used as an antifungal medicine that fights infections caused by fungus.
Nat Commun, 2024, 15(1):8708
Cell Rep Med, 2023, 4(12):101309
Int J Mol Sci, 2022, 23(22)13809
S0713 S107 hydrochloride S107 hydrochloride is a specific stabilizer of RyR2 (type 2 ryanodine receptor)/FKBP12.6 (FK506 binding protein 12.6) complex that affects Ca2+ signaling.
S3236 Mesaconitine Mesaconitine, one of the aconite alkaloids in Aconiti tuber, increases the [Ca2+]i level in endothelial cells by influx of Ca2+ from extracellular spaces.
S0973 Wilforgine Wilforgine, one of the major bioactive sesquiterpene alkaloids in Tripterygium wilfordii Hook. F., induces microstructural and ultrastructural changes in the muscles of M. separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system.
E0936 IGS-1.76 IGS-1.76, a protein-protein interaction (PPI) inhibitor, which exerts drug-like properties showing a significantly affinity for human neuronal calcium sensor 1 (hNCS-1), and efficiently modulates the interaction of hNCS-1 and guanine exchange factor Ric8a.
S3191 Azumolene Azumolene (EU4093 free base), an equipotent dantrolene analog, is a ryanodine receptor (RyR) modulator that inhibits the calcium-release.
S4353 Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
E4919New Barnidipine hydrochloride Barnidipine hydrochloride(Mepirodipine hydrochloride, YM-09730-5) is an antagonist of L-type calcium (CaA). It displays a high affinity for [3H] initrendipine binding sites with a Ki value of 0.21 nmol/l. Barnidipine hydrochloride also acts as an antihypertensive agent.
E4980New Verapamil Verapamil(Iproveratril,Dilacoran), is a phenylalkylamine derivative which is an antagonist of calcium influx and also an inhibitor P-gp and CYP3A4. It exhibits potency in treatment for angina, cardiac arrhythmias, cardiomyopathies and hypertension.

Calcium Channel阻害剤の選択性比較

Tags: Calcium Channel inhibitor|Calcium Channel agonist|Calcium Channel activator|Calcium Channel inducer|Calcium Channel antagonist|Calcium Channel signaling pathway|Calcium Channel assay kit