S2556 |
Rosiglitazone
|
Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis. |
-
Nat Commun, 2024, 15(1):1429
-
Nat Commun, 2024, 15(1):7991
-
Research (Wash D C), 2024, 7:0400
|
|
S8639 |
DPI (Diphenyleneiodonium chloride)
|
DPI (Diphenyleneiodonium chloride) is an inhibitor of NADPH oxidase and also a potent, irreversible, and time-, temperature-dependent iNOS/eNOS inhibitor. Diphenyleneiodonium chloride (DPI) also functions as a TRPA1 activator and selectively inhibits intracellular reactive oxygen species (ROS). |
-
Cell Death Discov, 2024, 10(1):122
-
Int Immunopharmacol, 2024, 143(Pt 2):113504
-
J Exp Clin Cancer Res, 2023, 42(1):236
|
|
S2505 |
Rosiglitazone maleate
|
Rosiglitazone maleate, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis. |
-
Stem Cell Reports, 2022, 17(11):2531-2547
-
Cell Death Dis, 2021, 12(11):972
-
Antioxidants (Basel), 2021, 10(2)155
|
|
S7999 |
SKF96365
|
SKF96365, originally identified as a blocker of receptor-mediated calcium entry, is widely used diagnostically, as a blocker of transient receptor potential canonical type (TRPC) channels. |
-
Research Square, 2024, 10.21203/rs.3.rs-3863076/v1
-
J Exp Clin Cancer Res, 2023, 42(1):195
-
J Exp Clin Cancer Res, 2023, 42(1):195
|
|
S7115 |
AMG-517
|
AMG 517 is a potent and selective TRPV1 antagonist, and antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM, respectively. |
-
Mucosal Immunol, 2024, S1933-0219(24)00006-0
-
iScience, 2023, 26(5):106749
-
Temperature (Austin), 2023, 10(1):136-154
|
|
S2918 |
HC-030031
|
HC-030031 (TOSLAB 829227) is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively. |
-
Lipids Health Dis, 2023, 22(1):6
-
Mol Pain, 2023, 19:17448069231158290
-
Int J Environ Res Public Health, 2022, 19(13)7985
|
|
S1990 |
Capsaicin(Vanilloid)
|
Capsaicin(Vanilloid) is an active component of chili peppers, which are plants belonging to the genus Capsicum.Capsaici is a TRPV1 agonist with an EC50 of 0.29 μM in HEK293 cells.Capsaicin is a mixture of Capsaicin and Dihydrocapsaicin. |
-
Invest Ophthalmol Vis Sci, 2024, 65(4):30
-
J Tradit Complement Med, 2024, 14(2):162-172
-
iScience, 2023, 26(5):106749
|
|
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
|
|
S8367 |
GSK2193874
|
GSK2193874 is an orally active, potent, and selective blocker of transient receptor potential vanilloid 4 (TRPV4) with IC50 values of 0.04 and 0.002 μM for hTRPV4 and rTRPV4, respectively. |
-
Int J Oral Sci, 2024, 16(1):3
-
iScience, 2023, 26(5):106749
-
Int J Mol Sci, 2023, 24(5)4926
|
|
S8137 |
Capsazepine
|
Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. If you want to do cell experiments, please select batch 01. |
-
J Ethnopharmacol, 2024, 337(Pt 2):118882
-
Sci Adv, 2023, 9(27):eadg9593
-
Neuron, 2022, S0896-6273(22)00954-0
|
|
S8107 |
GSK1016790A
|
GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells. |
-
Am J Physiol Lung Cell Mol Physiol, 2024, 326(3):L252-L265
-
iScience, 2023, 26(5):106749
-
Int J Mol Sci, 2023, 24(5)4926
|
|
S2773 |
SB705498
|
SB705498 is a TRPV1 antagonist for hTRPV1, antagonizes capsaicin, acid, and heat activation of TRPV1 with IC50 of 3 nM, 0.1 nM and 6 nM, shows a degree of voltage dependence, exhibits >100-fold selectivity for TRPV1 over TRPM8. Phase 2. |
-
Oxid Med Cell Longev, 2022, 2022:8096009
-
IUBMB Life, 2022, 10.1002/iub.2605
-
Biogerontology, 2016, 17(5-6):907-920
|
|
S2277 |
Caffeic Acid
|
Caffeic acid is a hydroxycinnamic acid, a naturally occurring organic compound. |
-
Molecules, 2021, 26(5)1210
-
J Nutr Biochem, 2015, 26(11):1379-84
-
Sci Rep, 2015, 5:12580
|
|
S4022 |
Probenecid
|
Probenecid (Benemid) is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. Probenecid is also a clinically used broad-spectrum Pannexin1 (Panx1) blocker. |
-
Mil Med Res, 2024, 11(1):41
-
Front Immunol, 2022, 13:992505
-
Vet World, 2022, 15(2):383-389
|
|
S6637 |
HC-067047
|
HC-067047 is a selective TRPV4 channel antagonist with IC50 values of 48 nM,133 nM,and 17 nM for human, rat, and mouse TRPV4 orthologs,respectively. |
-
Cell Physiol Biochem, 2024, 58(4):292-310
-
Front Pharmacol, 2023, 14:1101498
-
Cell Death Dis, 2020, 11(11):1009
|
|
S3763 |
Cinnamaldehyde
|
Cinnamaldehyde is a flavonoid that is naturally synthesized by the shikimate pathway. Its supplementation can improve glucose and lipid homeostasis in diabetic animals; a TRPA1 agonist. |
-
Int J Mol Sci, 2023, 24(11)9501
-
Int J Mol Sci, 2023, 24(11)9501
-
Biosci Rep, 2021, BSR20211828
|
|
S2650 |
RN-1734
|
RN-1734 (TRPV4 Antagonist I) is a selective transient receptor potential vanilloid 4 (TRPV4) antagonist with IC50 of 2.3 μM, 5.9 μM and 3.2 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1734 alleviates demyelination and inhibits glial activation and the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells. |
-
Theranostics, 2022, 12(4): 1621-1638
-
Theranostics, 2022, 12(4):1621-1638
|
|
S3942 |
Cardamonin
|
Cardamonin (Alpinetin chalcone), isolated from the fruits of Alpinia species, is a chalconoid with anti-inflammatory and anti-tumor activity. It has been shown to be a novel antagonist of hTRPA1 cation channel with IC50 of 454 nM while does not interact with TRPV1 nor TRPV4 channel. |
-
Cell, 2023, 186(13):2929-2949.e20
-
Food Funct, 2021, 12(23):11808-11818
|
|
S8691 |
ML204
|
ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC50 values of about 1 μM in fluorescent intracellular Ca2+ assays and about 3 μM in whole-cell voltage clamp experiments. It exhibits some selectivity within the TRPC subfamily of channels and higher selectivity against other TRP channels and non-TRP channels. |
-
Nature, 2019, 567(7747):262-266
|
|
S8238 |
SB366791
|
SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist. |
-
Mol Pain, 2018, 14:1744806918816850
|
|
S4714 |
(-)-Menthol
|
(-)-Menthol (L-Menthol, Levomenthol, Menthomenthol, Menthacamphor) is a levo isomer of menthol and used as a cooling agent that strongly activates TRPM8. |
-
Curr Biol, 2019, 29(11):1787-1799.e5
|
|
S6122 |
Cyclohexanecarboxamide
|
Cyclohexanecarboxamide (Ethyl menthane carboxamide, WS3, Hexahydrobenzamide) is a cooling agent and an agonist at TRPM8 receptors (EC50 = 3.7 μM). |
|
|
S6638 |
AMG-333
|
AMG-333 is a potent and highly selective antagonist of TRPM8 with IC50 values of 13 nM and 30 nM for human TRPM8 and rat TRPM8. |
|
|
E1890New |
A-967079
|
A-967079 is a selective antagonist of TRPA1 receptor with IC50 values of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively. A-967079 decreases the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation and high-intensity mechanical stimulation in rats. It demonstrates strong penetration into the central nervous system (CNS). |
|
|
S6947 |
MK6-83
|
MK6-83 is a novel Transient receptor potential melastatin member 1 (TRPML1) activator that may be used as a potential pharmacological treatment option for a specific subgroup of MLIV patients. |
|
|
E4659New |
Pyr3
|
Pyr3 is a selective and potent inhibitor of transient receptor potential canonical channel 3 (TRPC3). It inhibits TRPC3-mediated Ca2+ influx in a dose-dependent manner with the IC50 value of 0.7 μM. It holds potential for treating TRPC3-related diseases like cardiac hypertrophy. |
|
|
S0825 |
MDR-652
|
MDR-652 is a potent and specific agonist of transient receptor potential vanilloid 1 (TRPV1) with Ki of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively. MDR-652 has excellent and dose-dependent analgesic activity. |
|
|
S8073 |
Optovin
|
Optovin is a reversible photoactivated TRPA1 activator.
|
|
|
S9140 |
Pulegone
|
Pulegone, a naturally occurring organic compound, is a fragrance and flavour ingredient. |
|
|
S0750 |
GFB-8438
|
GFB-8438 is a novel, potent, and subtype selective TRP channel subfamily C (TRPC) inhibitor that is equipotent against TRPC4 and TRPC5 with IC50 of 0.18 μM and 0.29 μM, and shows excellent selectivity against TRPC6, other TRP family members , NaV 1.5, as well as limited activity against the hERG channel. |
|
|
S0977 |
AC1903
|
AC1903 (compound 2) is a specific and selective TRPC5 (transient receptor potential canonical channel 5) inhibitor with IC50 of 4.06 μM. |
-
Front Med (Lausanne), 2024, 11:1381479
|
|
S6634 |
SAR7334
|
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels.SAR7334 blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment. |
|
|
S7848 |
QX-314 chloride
|
QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels. |
|
|
E2871 |
Trovafloxacin Mesylate
|
Trovafloxacin mesylate, a broad-spectrum quinolone antibiotic, is a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. |
|
|
E2515 |
JT010
|
JT010 is a potent agonist of transient receptor potential cation channel subfamily A member 1 (TRPA1) with an EC50 of 0.65 nM. |
|
|
S3756 |
Methyl salicylate
|
Methyl salicylate (Betula oil, Gaultheria oil, Methyl 2-hydroxybenzoate, Natural wintergreen oil) is an organic ester naturally produced by many species of plants, particularly wintergreens. It is an agonist for TRPA1 and TRPV1. |
|
|
S6934 |
AMG-9810
|
AMG-9810 is a potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling. |
|
|
S6838 |
BCTC
|
BCTC is an orally effective and highly potent vanilloid receptor 1 (VR1/TRPV1) antagonist. BCTC inhibits capsaicin-induced and acid-induced activation of rat VR1 with IC50 of 35 nM and 6.0 nM, respectivley. BCTC exhibits anti-tumor activity. |
|
|
S6409 |
Zucapsaicin
|
Zucapsaicin, the cis-isomer of capsaicin, is a topical analgesic used to treat osteoarthritis of the knee and other neuropathic pain. It is also a TRPV-1 modulator. |
-
Arch Biochem Biophys, 2024, 754:109958
|
|
S6070 |
CBA (TRPM4-IN-5)
|
CBA (TRPM4-IN-5, Compound 5) is a highly selective blocker of the TRPM4 ion channel with an IC50 of 1.5μM. |
|
|
S6410 |
Clemizole
|
Clemizole, a first-generation histamine receptor (H1) antagonist, is a potent inhibitor of behavioural and electrographic seizure activity. It has a potential therapeutic effect on hepatitis C infection and also potently inhibits TRPC5 ion channels. |
|
|
S9086 |
Dihydrocapsaicin
|
Dihydrocapsaicin (6,7-Dihydrocapsaicin, 8-Methyl-N-vanillylnonanamide, CCRIS1589), found in pepper (C. annuum), is a potential nutriceutical. |
|
|
S0174 |
TRPM8 antagonist 2
|
TRPM8 antagonist 2 (TRPM8 Antagonist) is a potent and selective antagonist of TRPM8 with IC50 of 0.2 nM that can be used for the pharmacological treatment of neuropathic pain syndromes. |
|
|
E0028 |
9-Phenanthrol
|
9-Phenanthrol (9-Hydroxyphenanthrene, Phenanthren-9-o, 9-Phenanthrenol) is a selective TRPM4 inhibitor with an IC50 in the range of 0.02 μM, without effects on TRPM5. |
|
|
E0031 |
RN-1747
|
RN-1747 is a selective TRPV4 agonist with EC50s of 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1747 also antagonizes TRPM8 with IC50 of 4 μM. |
|
|
E0026 |
ML-SI3
|
ML-SI3 is a potent TRPML channel inhibitor with IC50s of 4.7 µM and 1.7 µM for TRPML1 and TRPML2, respectively. |
-
Mol Biol Cell, 2024, 35(5):ar70
|
|
S9926 |
ML-SA1
|
ML-SA1 (Mucolipin synthetic agonist 1) is an activator of TRPML channels. ML-SA1 also inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 values of ML-SA1 against DENV2 RNA and ZIKV RNA are 8.93 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral. |
|
|
S5419 |
1,4-Cineole
|
1,4-Cineole (Isocineole) is a widely distributed, natural, oxygenated monoterpene. 1,4-Cineole, present in eucalyptus oil, activates both human TRPM8 and human TRPA1. |
|
|
E2684 |
Icilin
|
Icilin is an agonist of the transient receptor potential M8 (TRPM8) ion channel with an EC50 of 1.4 μM. |
|
|
E4648New |
Pico145
|
Pico145(HC-608) is a selective inhibitor of TRPC1/4/5 channels. It inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50 values of 0.349 and 1.3 nM, respectively. It exhibits no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. |
|
|
S4787 |
Methyl syringate
|
Methyl syringate (Syringic Acid Methyl Ester), a plant phenolic compound, is a specific and selective TRPA1 agonist. |
|
|
S3851 |
Camphor
|
Camphor (2-Bornanone, Bornan-2-one, 2-Camphanone, Formosa) is a bicyclic monoterpene ketone found widely in plants, especially cinnamomum camphora and used topically as a skin antipruritic and as an anti-infective agent. |
-
iScience, 2023, 26(5):106749
|
|
S4516 |
(+)-Camphor
|
Camphor is a waxy, flammable, white or transparent solid with a strong aroma, often used to relieve pain, reduce itching and treat fungal infections. It can activate TRPV1 and TRPV3. |
|
|
S3867 |
(E)-Cardamonin
|
(E)-Cardamonin (Alpinetin chalcone, cardamomin) is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-κB inhibitor. |
|
|
S2963 |
WS-12
|
WS-12 is a potent TRPM8 agonist with an EC50 of 39 nM. |
|
|
E4673New |
AMTB hydrochloride
|
AMTB hydrochloride is a blocker of the transient receptor potential melastatin 8 (TRPM8) ion channel. It reduces the activation of TRPM8 channels induced by icilin, as assessed through a Ca2+ influx assay, with a pIC50 of 6.23. It is used as a tool to evaluate the role of this channel in bladder rhythmic contraction. |
|
|
S1990 |
Capsaicin(Vanilloid)
|
Capsaicin(Vanilloid) is an active component of chili peppers, which are plants belonging to the genus Capsicum.Capsaici is a TRPV1 agonist with an EC50 of 0.29 μM in HEK293 cells.Capsaicin is a mixture of Capsaicin and Dihydrocapsaicin. |
-
Invest Ophthalmol Vis Sci, 2024, 65(4):30
-
J Tradit Complement Med, 2024, 14(2):162-172
-
iScience, 2023, 26(5):106749
|
|
S4022 |
Probenecid
|
Probenecid (Benemid) is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. Probenecid is also a clinically used broad-spectrum Pannexin1 (Panx1) blocker. |
-
Mil Med Res, 2024, 11(1):41
-
Front Immunol, 2022, 13:992505
-
Vet World, 2022, 15(2):383-389
|
|
S3763 |
Cinnamaldehyde
|
Cinnamaldehyde is a flavonoid that is naturally synthesized by the shikimate pathway. Its supplementation can improve glucose and lipid homeostasis in diabetic animals; a TRPA1 agonist. |
-
Int J Mol Sci, 2023, 24(11)9501
-
Int J Mol Sci, 2023, 24(11)9501
-
Biosci Rep, 2021, BSR20211828
|
|
S6122 |
Cyclohexanecarboxamide
|
Cyclohexanecarboxamide (Ethyl menthane carboxamide, WS3, Hexahydrobenzamide) is a cooling agent and an agonist at TRPM8 receptors (EC50 = 3.7 μM). |
|
|
S0825 |
MDR-652
|
MDR-652 is a potent and specific agonist of transient receptor potential vanilloid 1 (TRPV1) with Ki of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively. MDR-652 has excellent and dose-dependent analgesic activity. |
|
|
E2515 |
JT010
|
JT010 is a potent agonist of transient receptor potential cation channel subfamily A member 1 (TRPA1) with an EC50 of 0.65 nM. |
|
|
S9086 |
Dihydrocapsaicin
|
Dihydrocapsaicin (6,7-Dihydrocapsaicin, 8-Methyl-N-vanillylnonanamide, CCRIS1589), found in pepper (C. annuum), is a potential nutriceutical. |
|
|
E0031 |
RN-1747
|
RN-1747 is a selective TRPV4 agonist with EC50s of 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1747 also antagonizes TRPM8 with IC50 of 4 μM. |
|
|
E2684 |
Icilin
|
Icilin is an agonist of the transient receptor potential M8 (TRPM8) ion channel with an EC50 of 1.4 μM. |
|
|
S4787 |
Methyl syringate
|
Methyl syringate (Syringic Acid Methyl Ester), a plant phenolic compound, is a specific and selective TRPA1 agonist. |
|
|
S2963 |
WS-12
|
WS-12 is a potent TRPM8 agonist with an EC50 of 39 nM. |
|
|
S7999 |
SKF96365
|
SKF96365, originally identified as a blocker of receptor-mediated calcium entry, is widely used diagnostically, as a blocker of transient receptor potential canonical type (TRPC) channels. |
- Research Square, 2024, 10.21203/rs.3.rs-3863076/v1
- J Exp Clin Cancer Res, 2023, 42(1):195
- J Exp Clin Cancer Res, 2023, 42(1):195
|
|
S2918 |
HC-030031
|
HC-030031 (TOSLAB 829227) is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively. |
- Lipids Health Dis, 2023, 22(1):6
- Mol Pain, 2023, 19:17448069231158290
- Int J Environ Res Public Health, 2022, 19(13)7985
|
|
S8367 |
GSK2193874
|
GSK2193874 is an orally active, potent, and selective blocker of transient receptor potential vanilloid 4 (TRPV4) with IC50 values of 0.04 and 0.002 μM for hTRPV4 and rTRPV4, respectively. |
- Int J Oral Sci, 2024, 16(1):3
- iScience, 2023, 26(5):106749
- Int J Mol Sci, 2023, 24(5)4926
|
|
S2277 |
Caffeic Acid
|
Caffeic acid is a hydroxycinnamic acid, a naturally occurring organic compound. |
- Molecules, 2021, 26(5)1210
- J Nutr Biochem, 2015, 26(11):1379-84
- Sci Rep, 2015, 5:12580
|
|
S8691 |
ML204
|
ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC50 values of about 1 μM in fluorescent intracellular Ca2+ assays and about 3 μM in whole-cell voltage clamp experiments. It exhibits some selectivity within the TRPC subfamily of channels and higher selectivity against other TRP channels and non-TRP channels. |
- Nature, 2019, 567(7747):262-266
|
|
E4659New |
Pyr3
|
Pyr3 is a selective and potent inhibitor of transient receptor potential canonical channel 3 (TRPC3). It inhibits TRPC3-mediated Ca2+ influx in a dose-dependent manner with the IC50 value of 0.7 μM. It holds potential for treating TRPC3-related diseases like cardiac hypertrophy. |
|
|
S9140 |
Pulegone
|
Pulegone, a naturally occurring organic compound, is a fragrance and flavour ingredient. |
|
|
S0750 |
GFB-8438
|
GFB-8438 is a novel, potent, and subtype selective TRP channel subfamily C (TRPC) inhibitor that is equipotent against TRPC4 and TRPC5 with IC50 of 0.18 μM and 0.29 μM, and shows excellent selectivity against TRPC6, other TRP family members , NaV 1.5, as well as limited activity against the hERG channel. |
|
|
S0977 |
AC1903
|
AC1903 (compound 2) is a specific and selective TRPC5 (transient receptor potential canonical channel 5) inhibitor with IC50 of 4.06 μM. |
- Front Med (Lausanne), 2024, 11:1381479
|
|
S6634 |
SAR7334
|
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels.SAR7334 blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment. |
|
|
E2871 |
Trovafloxacin Mesylate
|
Trovafloxacin mesylate, a broad-spectrum quinolone antibiotic, is a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. |
|
|
S6070 |
CBA (TRPM4-IN-5)
|
CBA (TRPM4-IN-5, Compound 5) is a highly selective blocker of the TRPM4 ion channel with an IC50 of 1.5μM. |
|
|
S6410 |
Clemizole
|
Clemizole, a first-generation histamine receptor (H1) antagonist, is a potent inhibitor of behavioural and electrographic seizure activity. It has a potential therapeutic effect on hepatitis C infection and also potently inhibits TRPC5 ion channels. |
|
|
E0028 |
9-Phenanthrol
|
9-Phenanthrol (9-Hydroxyphenanthrene, Phenanthren-9-o, 9-Phenanthrenol) is a selective TRPM4 inhibitor with an IC50 in the range of 0.02 μM, without effects on TRPM5. |
|
|
E0026 |
ML-SI3
|
ML-SI3 is a potent TRPML channel inhibitor with IC50s of 4.7 µM and 1.7 µM for TRPML1 and TRPML2, respectively. |
- Mol Biol Cell, 2024, 35(5):ar70
|
|
E4648New |
Pico145
|
Pico145(HC-608) is a selective inhibitor of TRPC1/4/5 channels. It inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50 values of 0.349 and 1.3 nM, respectively. It exhibits no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. |
|
|
S7115 |
AMG-517
|
AMG 517 is a potent and selective TRPV1 antagonist, and antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM, respectively. |
- Mucosal Immunol, 2024, S1933-0219(24)00006-0
- iScience, 2023, 26(5):106749
- Temperature (Austin), 2023, 10(1):136-154
|
|
S8137 |
Capsazepine
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Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. If you want to do cell experiments, please select batch 01. |
- J Ethnopharmacol, 2024, 337(Pt 2):118882
- Sci Adv, 2023, 9(27):eadg9593
- Neuron, 2022, S0896-6273(22)00954-0
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S2773 |
SB705498
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SB705498 is a TRPV1 antagonist for hTRPV1, antagonizes capsaicin, acid, and heat activation of TRPV1 with IC50 of 3 nM, 0.1 nM and 6 nM, shows a degree of voltage dependence, exhibits >100-fold selectivity for TRPV1 over TRPM8. Phase 2. |
- Oxid Med Cell Longev, 2022, 2022:8096009
- IUBMB Life, 2022, 10.1002/iub.2605
- Biogerontology, 2016, 17(5-6):907-920
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S6637 |
HC-067047
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HC-067047 is a selective TRPV4 channel antagonist with IC50 values of 48 nM,133 nM,and 17 nM for human, rat, and mouse TRPV4 orthologs,respectively. |
- Cell Physiol Biochem, 2024, 58(4):292-310
- Front Pharmacol, 2023, 14:1101498
- Cell Death Dis, 2020, 11(11):1009
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S2650 |
RN-1734
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RN-1734 (TRPV4 Antagonist I) is a selective transient receptor potential vanilloid 4 (TRPV4) antagonist with IC50 of 2.3 μM, 5.9 μM and 3.2 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1734 alleviates demyelination and inhibits glial activation and the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells. |
- Theranostics, 2022, 12(4): 1621-1638
- Theranostics, 2022, 12(4):1621-1638
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S3942 |
Cardamonin
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Cardamonin (Alpinetin chalcone), isolated from the fruits of Alpinia species, is a chalconoid with anti-inflammatory and anti-tumor activity. It has been shown to be a novel antagonist of hTRPA1 cation channel with IC50 of 454 nM while does not interact with TRPV1 nor TRPV4 channel. |
- Cell, 2023, 186(13):2929-2949.e20
- Food Funct, 2021, 12(23):11808-11818
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S8238 |
SB366791
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SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist. |
- Mol Pain, 2018, 14:1744806918816850
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S6638 |
AMG-333
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AMG-333 is a potent and highly selective antagonist of TRPM8 with IC50 values of 13 nM and 30 nM for human TRPM8 and rat TRPM8. |
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E1890New |
A-967079
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A-967079 is a selective antagonist of TRPA1 receptor with IC50 values of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively. A-967079 decreases the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation and high-intensity mechanical stimulation in rats. It demonstrates strong penetration into the central nervous system (CNS). |
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S3756 |
Methyl salicylate
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Methyl salicylate (Betula oil, Gaultheria oil, Methyl 2-hydroxybenzoate, Natural wintergreen oil) is an organic ester naturally produced by many species of plants, particularly wintergreens. It is an agonist for TRPA1 and TRPV1. |
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S6934 |
AMG-9810
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AMG-9810 is a potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling. |
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S6838 |
BCTC
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BCTC is an orally effective and highly potent vanilloid receptor 1 (VR1/TRPV1) antagonist. BCTC inhibits capsaicin-induced and acid-induced activation of rat VR1 with IC50 of 35 nM and 6.0 nM, respectivley. BCTC exhibits anti-tumor activity. |
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S0174 |
TRPM8 antagonist 2
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TRPM8 antagonist 2 (TRPM8 Antagonist) is a potent and selective antagonist of TRPM8 with IC50 of 0.2 nM that can be used for the pharmacological treatment of neuropathic pain syndromes. |
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S3867 |
(E)-Cardamonin
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(E)-Cardamonin (Alpinetin chalcone, cardamomin) is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-κB inhibitor. |
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