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TRP Channel Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
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
Front Immunol, 2024, 15:1477072
iScience, 2023, 26(5):106749
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.
Biol Pharm Bull, 2025, 48(6):769-781
J Ethnopharmacol, 2024, 337(Pt 2):118882
Sci Adv, 2023, 9(27):eadg9593
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
Verified customer review of SB705498
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 Oncol (Dordr), 2024, 10.1007/s13402-024-01008-7
Cell Physiol Biochem, 2024, 58(4):292-310
Front Pharmacol, 2023, 14:1101498
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 this compound does not interact with TRPV1 nor TRPV4 channel.
Cell, 2023, 186(13):2929-2949.e20
Food Funct, 2021, 12(23):11808-11818
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. This compound 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
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. This compound blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. It significantly reduces the mRNA expression of TLR2 and TLR4. This chemical also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.
Int J Mol Sci, 2025, 26(18)8816
S8238 SB366791 SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist with an IC50 of 5.7 nM.
Mol Pain, 2018, 14:1744806918816850
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.
E1890 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. This compound 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).
E5813 JNJ-28583113 JNJ-28583113 is a potent, brain-penetrant antagonist of TRPM2 with an IC50 of 126 nM that protects cells from oxidative stress-induced death and morphological changes. It also inhibits microglial cytokine release in response to pro-inflammatory stimuli and promotes GSK3α/β phosphorylation.
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.
S6838 BCTC BCTC is an orally effective and highly potent vanilloid receptor 1 (VR1/TRPV1) antagonist. This compound inhibits capsaicin-induced and acid-induced activation of rat VR1 with IC50 of 35 nM and 6.0 nM, respectivley. It exhibits anti-tumor activity.
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.
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.