• TRPV
  • TRPA
  • TRPC
  • TRPM
  • TRPML

TRPV Selective Inhibitors | Activators | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
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. Selective TRPV1, IC50: 1 nM-2 nM
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. Selective rTRPV4, IC50: 0.002 μM; hTRPV4, IC50: 0.04 μM
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. Selective hTRPV4, IC50: 2.1 nM; mTRPV4, IC50: 18 nM
S8238 SB366791 SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist with an IC50 of 5.7 nM. Selective TRPV1, IC50: 5.7 nM
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. Selective rTRPV1 (acid-induced), IC50: 6.0 nM; rTRPV1 (capsaicin-induced), IC50: 35 nM
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. Selective rTRPV1, Ki: 23.8 nM; hTRPV1, Ki: 11.4 nM
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. Selective mTRPV4, IC50: 17 nM; rTRPV4, IC50: 133 nM; hTRPV4, IC50: 48 nM
S6934 AMG-9810 AMG-9810 is 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 tumorigenes Selective rTRPV1, IC50: 85.6 nM; hTRPV1, IC50: 24.5 nM
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. Selective hTRPV1, pKi: 7.6; hTRPV1, pIC50: 7.1
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. Selective rTRPV4, IC50: 3.2 μM; mTRPV4, IC50: 5.9 μM; hTRPV4, IC50: 2.3 μM
S8137 Capsazepine Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. Selective
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. Selective
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. Selective
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. Pan
S7848 QX-314 chloride QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels. Pan