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	hTRPV4, IC50: 0.04 μM; rTRPV4, IC50: 0.002 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	mTRPV4, IC50: 18 nM; hTRPV4, IC50: 2.1 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 (capsaicin-induced), IC50: 35 nM; rTRPV1 (acid-induced), IC50: 6.0 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	hTRPV1, Ki: 11.4 nM; rTRPV1, Ki: 23.8 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	hTRPV4, IC50: 48 nM; rTRPV4, IC50: 133 nM; mTRPV4, IC50: 17 nM
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 tumorigen	Selective	hTRPV1, IC50: 24.5 nM; rTRPV1, IC50: 85.6 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, pIC50: 7.1; hTRPV1, pKi: 7.6
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	hTRPV4, IC50: 2.3 μM; mTRPV4, IC50: 5.9 μM; rTRPV4, IC50: 3.2 μM
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
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
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.	Selective
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
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