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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M6494 | BCTC | BCTC is a tRPV1 antagonist. BCTC is also a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells. |
| M7698 | Capsazepine | Capsazepine is a specific vanilloid receptor antagonist; synthetic analog of capsaicin. |
| M10315 | MK6-83 | MK6-83 is an agonist of the transient receptor potential channel ML3 (TRPML3). |
| M9962 | Nonivamide | Nonivamide (also called pelargonic acid vanillylamide or PAVA) can activate the TRPV1 receptor, thus, stimulate the firing rate of dopaminergic neurons in the ventral tegmental area of the brain and to increase the expression of the serotonin receptor gene HTR2A. |
| M2960 | Probenecid | Probenecid is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. |
| M21479 | Vocacapsaicin hydrochloride | Vocacapsaicin (CA-008) hydrochloride, as a prodrug of capsaicin, is the first non-opioid TRPV1 agonist. Vocacapsaicin hydrochloride provides lasting pain relief. |
| M21477 | Vocacapsaicin | Vocacapsaicin (CA-008), a prodrug of capsaicin, is the first (first-in-class) non-opioid TRPV1 agonist. Vocacapsaicin can provide lasting pain relief. |
| M21130 | GDC-0334 | GDC-0334 is a TRPA1 antagonist for the treatment of TRPA1-mediated disease and is an oral candidate compound for the study of asthma. |
| M20954 | 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. |
| M20832 | 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. |
| M20815 | WS-12 | WS-12 is a potent TRPM8 agonist with an EC50 of 39 nM. |
| M14288 | TRPC6-IN-1 | TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM. |
| M14287 | Resolvin D2 | Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. |
| M14286 | Pyr3 | Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700 nM for TRPC3-mediated Ca2+ influx. |
| M14285 | Pyr10 | Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. |
| M14284 | Pico145 | Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. |
| M14283 | PF-4840154 | PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse. |
| M14282 | ML204 hydrochloride | ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca2+ channels. |
| M14281 | HC-070 | HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively. |
| M14280 | GSK2798745 | GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. |
| M14279 | GSK205 | GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19 μM for inhibiting TRPV4-mediated Ca2+ influx. |
| M14278 | EIPA hydrochloride | EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also inhibits Na+/H+-exchanger (NHE) and macropinocytosis. |
| M14277 | BI-749327 | BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. |
| M14276 | A-1165442 | A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1. |
| M11223 | TRPM4-IN-1 | Trpm4-in-1 (CBA) is an effective and selective cationic channel TRPM4 inhibitor with an IC50 of 1.5 μM. |
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