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Calcium Channel
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Calcium Channel製品
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- Calcium Channel阻害剤 (71)
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- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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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. |
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| 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). | ||
| 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. |
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| S1808 | Nifedipine | Nifedipine is a dihydropyridine calcium channel blocker, used to lower hypertension and to treat angina. |
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| S2721 | Nilvadipine | Nilvadipine (ARC029, FR34235,FK235) is a potent calcium channel blocker with an IC50 of 0.03 nM. | ||
| 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. | ||
| S1905 | Amlodipine | Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain. | ||
| 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. | ||
| S1293 | Cilnidipine | Cilnidipine is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment. | ||
| 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. | ||
| 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. |
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| 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. | ||
| S7924 | Bay K 8644 | Bay K 8644 is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM. |
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| 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. | ||
| S1662 | Isradipine | Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure. | ||
| 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). |
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| 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. | ||
| S1813 | Amlodipine Besylate | Amlodipine Besylate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain. | ||
| 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. | ||
| 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. |
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| S1885 | Felodipine | Felodipine (CGH-869) is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM. | ||
| S1747 | Nimodipine | Nimodipine (BAY E 9736) is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure. |
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| S2017 | Benidipine HCl | Benidipine HCl (KW-3049,(±)- Benidipine) is a hydrochloride salt form of benidipine which is a dihydropyridine calcium channel blocker. | ||
| 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. | ||
| 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. | ||
| S1799 | Ranolazine | Ranolazine (CVT 303, RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina. | ||
| S2535 | Econazole nitrate | Econazole Nitrate (NSC 243115,Spectazole) is a Ca2+ channel blocker, used as an antifungal medicine that fights infections caused by fungus. | ||
| S4181 | Nicardipine HCl | Nicardipine HCl (RS-69216,YC-93) is a dihydropyridine calcium-channel blocking agent used for the treatment of vascular disorders. | ||
| S3053 | Azelnidipine | Azelnidipine (UR-12592) is a dihydropyridine calcium channel blocker. | ||
| 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. |
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| S2397 | Palmatine chloride | Palmatine hydrochloride (Palmatine chloride (6CI,7CI); Fibrauretin) is a hydrochloride salt of palmatine which is a protoberberine alkaloid. | ||
| 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. | ||
| 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. | ||
| S2481 | Manidipine | Manidipine(CV-4093,(±)-Manidipine) is a calcium channel blocker (dihydropyridine type) that is used clinically as an antihypertensive. | ||
| 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. |
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| S2080 | Clevidipine Butyrate | Clevidipine Butyrate(Cleviprex) is a dihydropyridine calcium channel blocker, uses as an agent for the reduction of blood pressure. | ||
| 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. | ||
| S5255 | Nicardipine | Nicardipine is a potent calcium channel blockader with marked vasodilator action. | ||
| S4626 | Ethosuximide | Ethosuximide(Zarontin) is a succinimide anticonvulsant, used mainly in absence seizures; A calcium channel blocker. |
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| S5966 | Amlodipine maleate | Amlodipine (Amvaz, UK-48340) maleate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain. | ||
| S4597 | Lercanidipine hydrochloride | Lercanidipine is a calcium channel blocker of the dihydropyridine class. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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). | ||
| 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. | ||
| 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. | ||
| S4727 | Cinnarizine | Cinnarizine (Stugeron, Dimitronal, Stutgin, Cinarizine) is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker. | ||
| 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. | ||
| 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. | ||
| E1879New | CBD3063 | CBD3063(EX-A8428) is a selective, first-in-class inhibitor of Cav2.2-CRMP2 (ollapsin response mediator protein 2)interaction. It suppresses surface trafficking of Cav2.2, and N-type (Cav2.2) calcium currents. CBD3063 allosterically regulates Cav2.2 to achieve analgesia and pain relief without negative side effect profiles. | ||
| 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. |
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| 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. | ||
| 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. | ||
| 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. |
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| 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). | ||
| 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. |
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| S1808 | Nifedipine | Nifedipine is a dihydropyridine calcium channel blocker, used to lower hypertension and to treat angina. |
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| S2721 | Nilvadipine | Nilvadipine (ARC029, FR34235,FK235) is a potent calcium channel blocker with an IC50 of 0.03 nM. | ||
| 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. | ||
| S1905 | Amlodipine | Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain. | ||
| 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. | ||
| S1293 | Cilnidipine | Cilnidipine is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment. | ||
| 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. | ||
| 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. |
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| 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. | ||
| S1662 | Isradipine | Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure. | ||
| 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). |
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| S1813 | Amlodipine Besylate | Amlodipine Besylate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain. | ||
| 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. | ||
| 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. |
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| S1885 | Felodipine | Felodipine (CGH-869) is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM. | ||
| S1747 | Nimodipine | Nimodipine (BAY E 9736) is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure. |
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| S2017 | Benidipine HCl | Benidipine HCl (KW-3049,(±)- Benidipine) is a hydrochloride salt form of benidipine which is a dihydropyridine calcium channel blocker. | ||
| 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. | ||
| S1799 | Ranolazine | Ranolazine (CVT 303, RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina. | ||
| S4181 | Nicardipine HCl | Nicardipine HCl (RS-69216,YC-93) is a dihydropyridine calcium-channel blocking agent used for the treatment of vascular disorders. | ||
| S3053 | Azelnidipine | Azelnidipine (UR-12592) is a dihydropyridine calcium channel blocker. | ||
| 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. |
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| 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. | ||
| 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. | ||
| S2481 | Manidipine | Manidipine(CV-4093,(±)-Manidipine) is a calcium channel blocker (dihydropyridine type) that is used clinically as an antihypertensive. | ||
| S2080 | Clevidipine Butyrate | Clevidipine Butyrate(Cleviprex) is a dihydropyridine calcium channel blocker, uses as an agent for the reduction of blood pressure. | ||
| 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. | ||
| S5255 | Nicardipine | Nicardipine is a potent calcium channel blockader with marked vasodilator action. | ||
| S4626 | Ethosuximide | Ethosuximide(Zarontin) is a succinimide anticonvulsant, used mainly in absence seizures; A calcium channel blocker. |
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| S5966 | Amlodipine maleate | Amlodipine (Amvaz, UK-48340) maleate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain. | ||
| S4597 | Lercanidipine hydrochloride | Lercanidipine is a calcium channel blocker of the dihydropyridine class. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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). | ||
| 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. | ||
| S4727 | Cinnarizine | Cinnarizine (Stugeron, Dimitronal, Stutgin, Cinarizine) is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker. | ||
| 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. | ||
| 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. | ||
| E1879New | CBD3063 | CBD3063(EX-A8428) is a selective, first-in-class inhibitor of Cav2.2-CRMP2 (ollapsin response mediator protein 2)interaction. It suppresses surface trafficking of Cav2.2, and N-type (Cav2.2) calcium currents. CBD3063 allosterically regulates Cav2.2 to achieve analgesia and pain relief without negative side effect profiles. | ||
| 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. |
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| 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. | ||
| 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. |
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| 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. | ||
| 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. | ||
| 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. | ||
| S2535 | Econazole nitrate | Econazole Nitrate (NSC 243115,Spectazole) is a Ca2+ channel blocker, used as an antifungal medicine that fights infections caused by fungus. | ||
| 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. | ||
| E1879New | CBD3063 | CBD3063(EX-A8428) is a selective, first-in-class inhibitor of Cav2.2-CRMP2 (ollapsin response mediator protein 2)interaction. It suppresses surface trafficking of Cav2.2, and N-type (Cav2.2) calcium currents. CBD3063 allosterically regulates Cav2.2 to achieve analgesia and pain relief without negative side effect profiles. | ||
| 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
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