TRP Channel Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S4022	Probenecid	Probenecid (Benemid) is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. This compound is also a clinically used broad-spectrum Pannexin1 (Panx1) blocker.	BMC Vet Res, 2025, 21(1):237 Mil Med Res, 2024, 11(1):41 Front Immunol, 2022, 13:992505
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
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.	J Biol Chem, 2025, 301(10):110716 bioRxiv, 2025, 2025.06.11.659112 Sci Rep, 2024, 14(1):24836
S2277	Caffeic Acid	Caffeic acid is a hydroxycinnamic acid, a naturally occurring organic compound. Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO).	Molecules, 2021, 26(5)1210 J Nutr Biochem, 2015, 26(11):1379-84 Sci Rep, 2015, 5:12580
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.	Bioact Mater, 2025, 43:240-254 Int J Mol Sci, 2023, 24(11)9501 Biosci Rep, 2021, BSR20211828
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
S6634	SAR7334	SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels. This compound blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment.	Adv Healthc Mater, 2025, e2404767. Nat Commun, 2024, 15(1):10476
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
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
S8073	Optovin	Optovin is a reversible photoactivated TRPA1 activator.	Cancer Drug Resist, 2025, 8:45
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
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
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
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.	Theranostics, 2025, 15(14):6901-6918
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
S9926	ML-SA1	ML-SA1 (Mucolipin synthetic agonist 1) is an activator of TRPML channels. This compound also inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 values of this chemical against DENV2 RNA and ZIKV RNA are 8.93 μM and 52.99 μM, respectively. It induces autophagy. It can be used for the research of broad-spectrum antiviral.	Sci Rep, 2024, 14(1):24836
E4648	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.	Biol Pharm Bull, 2025, 48(9):1444-1455
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
S4714	(-)-Menthol	(-)-Menthol 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.
E5869^New	ML-SA5	ML-SA5 is a potent agonist of TRPML1 cation channel that activates the entire endosomal TRPML1 (ML1) current in DMD myocytes with an EC50 of 285 nM and exhibit anticancer activity.
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).
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.
E4659	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. This compound has excellent and dose-dependent analgesic activity.
S9140	Pulegone	Pulegone, a naturally occurring organic compound, is a fragrance and flavour ingredient.pulegone stimulates both TRPM8 and TRPA1 channel in chicken sensory neurons and suppresses the former but not the latter at high concentrations.
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.
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.
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.
E0390^New	CIM0216	CIM0216 is a synthetic TRPM3 ligand that functions as a TRPM3 agonist. It shows preference for TRPM3 compared to TRPM1, TRPM2, and TRPM4-8. In vitro studies demonstrate that CIM0216 operates through TRPM3 to trigger pain responses and stimulate neuropeptide release from sensory nerve endings. This compound serves as a valuable research tool for investigating TRPM3's physiological roles and studying neurogenic inflammation.
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.
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.
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	Dihydrocapsiacin (6,7-Dihydrocapsaicin, 8-Methyl-N-vanillylnonanamide, CCRIS1589), found in pepper (C. annuum), is a potential nutriceutical. This compound is a selective TRPV1 agonist.
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.
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. This compound also antagonizes TRPM8 with IC50 of 4 μM.
S5419	1,4-Cineole	1,4-Cineole (Isocineole) is a widely distributed, natural, oxygenated monoterpene. This compound, 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.
S4787	Methyl syringate	Methyl syringate (Syringic Acid Methyl Ester), a plant phenolic compound, is a specific and selective TRPA1 agonist.
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.
S2963	WS-12	WS-12 is a potent TRPM8 agonist with an EC50 of 39 nM.
E4673	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.
S2556	Rosiglitazone (BRL 49653)	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.	Signal Transduct Target Ther, 2025, 10(1):394 Nat Commun, 2025, 16(1):6241 Lab Invest, 2025, 105(4):104103
S8639	DPI (Diphenyleneiodonium chloride)	Diphenyleneiodonium chloride (DPI) is an inhibitor of NADPH oxidase and also a potent, irreversible, and time-, temperature-dependent iNOS/eNOS inhibitor. It also functions as a TRPA1 activator and selectively inhibits intracellular reactive oxygen species (ROS).	Redox Biol, 2025, 80:103485 Sci Adv, 2025, 11(34):eadv6937 Exp Mol Med, 2024, 56(12):2602-2616
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. This compound also modulates TRP channels and induces autophagy. It prevents ferroptosis.	Stem Cell Reports, 2022, 17(11):2531-2547 Cell Death Dis, 2021, 12(11):972 Antioxidants (Basel), 2021, 10(2)155
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.