TRP Channel

Choose Selective TRP Channel Inhibitors

TRP Channel Products

  • All (52)
  • TRP Channel Inhibitors (13)
  • TRP Channel Activators (11)
  • TRP Channel Antagonists (13)
  • TRP Channel Agonists (12)
  • TRP Channel Modulators (3)
  • New TRP Channel Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0026New 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.

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.

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.
S0977 AC1903 AC1903 (compound 2) is a specific and selective TRPC5 (transient receptor potential canonical channel 5) inhibitor with IC50 of 4.06 μM.
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
S2918 HC-030031 HC-030031 (TOSLAB 829227) is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively.
Evid Based Complement Alternat Med, 2022, 2022:7464147
Exp Cell Res, 2021, S0014-4827(21)00330-X
Int Immunopharmacol, 2020, 86:106696
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.
S6634 SAR7334 SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels.SAR7334 blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment.
S7999 SKF96365 SKF96365, originally identified as a blocker of receptor-mediated calcium entry, is widely used diagnostically, as a blocker of transient receptor potential canonical type (TRPC) channels.
Front Pharmacol, 2021, 12:622774
J Agric Food Chem, 2021, 69(29):8144-8159
Biochim Biophys Acta Mol Cell Biol Lipids, 2020, 1865(12):158793
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.
Neurosci Bull, 2021, 10.1007/s12264-021-00662-3
Cell Prolif, 2020, 53(10):e12912
Toxicol Sci, 2019, 168(1):160-170
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
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.
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.
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.
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
S5419 1,4-Cineole 1,4-Cineole (Isocineole) is a widely distributed, natural, oxygenated monoterpene. 1,4-Cineole, present in eucalyptus oil, activates both human TRPM8 and human TRPA1.
S6657 2-Aminoethyl Diphenylborinate (2-APB) 2-Aminoethyl Diphenylborinate (2-APB) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations.
Int J Biol Sci, 2021, 17(13):3672-3688
Int J Biol Sci, 2021, 17(13):3672-3688
Chem Biol Interact, 2021, 351:109756
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.
S7848 QX-314 chloride QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels.
S8073 Optovin Optovin is a reversible photoactivated TRPA1 activator.
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.
Theranostics, 2022, 12(4): 1621-1638
Immunity, 2021, S1074-7613(21)00289-2
Cell Death Dis, 2020, 11(11):1009
S8639 Diphenyleneiodonium chloride (DPI) Diphenyleneiodonium chloride (DPI) is an inhibitor of NADPH oxidase and also a potent, irreversible, and time-, temperature-dependent iNOS/eNOS inhibitor. Diphenyleneiodonium chloride (DPI) also functions as a TRPA1 activator and selectively inhibits intracellular reactive oxygen species (ROS).
Nat Biotechnol, 2022, 10.1038/s41587-021-01169-y
Immunity, 2022, 55(7):1185-1199.e8
Bioeng Transl Med, 2022, 7(2):e10276
S9926 ML-SA1

ML-SA1 (Mucolipin synthetic agonist 1) is an activator of TRPML channels. ML-SA1 also inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 values of ML-SA1 against DENV2 RNA and ZIKV RNA are 8.93 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral.

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.
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.
Theranostics, 2022, 12(4): 1621-1638
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
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.
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-kB inhibitor.
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 does not interact with TRPV1 nor TRPV4 channel.
Food Funct, 2021, 12(23):11808-11818
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 Death Dis, 2020, 11(11):1009
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.
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.
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 tumorigenesis mediated through EGFR/Akt/mTOR signaling.
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, 2022, 10.1038/s41385-022-00533-8
Inflammation, 2019, 10.1007/s10753-019-01040-y
Mol Pain, 2018, 14:1744806918777614
S8137 Capsazepine Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist.
J Ethnopharmacol, 2022, 291:115157
Int J Mol Sci, 2021, 22(11)5551
Chem Biol Interact, 2021, 351:109756
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
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. RN-1747 also antagonizes TRPM8 with IC50 of 4 μM.

E2515New JT010 JT010 is a potent agonist of transient receptor potential cation channel subfamily A member 1 (TRPA1) with an EC50 of 0.65 nM.
E2684New Icilin Icilin is an agonist of the transient receptor potential M8 (TRPM8) ion channel with an EC50 of 1.4 μM.
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.
S1990 Capsaicin(Vanilloid) Capsaicin (Qutenza, Vanilloid) is an active component of chili peppers, which are plants belonging to the genus Capsicum. Capsaici is a TRPV1 agonist with an EC50 of 0.29 μM in HEK293 cells.
Oxid Med Cell Longev, 2022, 2022:8096009
Mar Drugs, 2022, 20(6)378
Neuroscience, 2021, S0306-4522(21)00641-2
S2963 WS-12 WS-12 is a potent TRPM8 agonist with an EC50 of 39 nM.
S3605 Borneol Borneol is a bicyclic monoterpenoid compound extracted from medicinal plants such as Blumea balsamifera, and Dryobalanops aromatica. It is a TRPM8 agonist that increases ocular surface wetness.
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.
Biosci Rep, 2021, BSR20211828
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.
S4787 Methyl syringate Methyl syringate (Syringic Acid Methyl Ester), a plant phenolic compound, is a specific and selective TRPA1 agonist.
S6122 Cyclohexanecarboxamide Cyclohexanecarboxamide (Ethyl menthane carboxamide, WS3, Hexahydrobenzamide) is a cooling agent and an agonist at TRPM8 receptors (EC50 = 3.7 μM).
S9086 Dihydrocapsaicin Dihydrocapsaicin (6,7-Dihydrocapsaicin, 8-Methyl-N-vanillylnonanamide, CCRIS1589), found in pepper (C. annuum), is a potential nutriceutical.DHC is a selective TRPV1 agonist.
S2505 Rosiglitazone (BRL-49653) maleate Rosiglitazone maleate (BRL 49653), 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. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
Front Cardiovasc Med, 2021, 8:698056
S2556 Rosiglitazone (BRL 49653) Rosiglitazone (BRL 49653) 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.
Redox Biol, 2022, 50:102256
Cancer Commun (Lond), 2022, 10.1002/cac2.12332
Free Radic Biol Med, 2022, 189:42-57
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.
E0026New 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.

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.

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.
S0977 AC1903 AC1903 (compound 2) is a specific and selective TRPC5 (transient receptor potential canonical channel 5) inhibitor with IC50 of 4.06 μM.
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
S2918 HC-030031 HC-030031 (TOSLAB 829227) is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively.
Evid Based Complement Alternat Med, 2022, 2022:7464147
Exp Cell Res, 2021, S0014-4827(21)00330-X
Int Immunopharmacol, 2020, 86:106696
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.
S6634 SAR7334 SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels.SAR7334 blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment.
S7999 SKF96365 SKF96365, originally identified as a blocker of receptor-mediated calcium entry, is widely used diagnostically, as a blocker of transient receptor potential canonical type (TRPC) channels.
Front Pharmacol, 2021, 12:622774
J Agric Food Chem, 2021, 69(29):8144-8159
Biochim Biophys Acta Mol Cell Biol Lipids, 2020, 1865(12):158793
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.
Neurosci Bull, 2021, 10.1007/s12264-021-00662-3
Cell Prolif, 2020, 53(10):e12912
Toxicol Sci, 2019, 168(1):160-170
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
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.
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.
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.
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
S5419 1,4-Cineole 1,4-Cineole (Isocineole) is a widely distributed, natural, oxygenated monoterpene. 1,4-Cineole, present in eucalyptus oil, activates both human TRPM8 and human TRPA1.
S6657 2-Aminoethyl Diphenylborinate (2-APB) 2-Aminoethyl Diphenylborinate (2-APB) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations.
Int J Biol Sci, 2021, 17(13):3672-3688
Int J Biol Sci, 2021, 17(13):3672-3688
Chem Biol Interact, 2021, 351:109756
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.
S7848 QX-314 chloride QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels.
S8073 Optovin Optovin is a reversible photoactivated TRPA1 activator.
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.
Theranostics, 2022, 12(4): 1621-1638
Immunity, 2021, S1074-7613(21)00289-2
Cell Death Dis, 2020, 11(11):1009
S8639 Diphenyleneiodonium chloride (DPI) Diphenyleneiodonium chloride (DPI) is an inhibitor of NADPH oxidase and also a potent, irreversible, and time-, temperature-dependent iNOS/eNOS inhibitor. Diphenyleneiodonium chloride (DPI) also functions as a TRPA1 activator and selectively inhibits intracellular reactive oxygen species (ROS).
Nat Biotechnol, 2022, 10.1038/s41587-021-01169-y
Immunity, 2022, 55(7):1185-1199.e8
Bioeng Transl Med, 2022, 7(2):e10276
S9926 ML-SA1

ML-SA1 (Mucolipin synthetic agonist 1) is an activator of TRPML channels. ML-SA1 also inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 values of ML-SA1 against DENV2 RNA and ZIKV RNA are 8.93 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral.

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.
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.
Theranostics, 2022, 12(4): 1621-1638
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
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.
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-kB inhibitor.
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 does not interact with TRPV1 nor TRPV4 channel.
Food Funct, 2021, 12(23):11808-11818
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 Death Dis, 2020, 11(11):1009
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.
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.
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 tumorigenesis mediated through EGFR/Akt/mTOR signaling.
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, 2022, 10.1038/s41385-022-00533-8
Inflammation, 2019, 10.1007/s10753-019-01040-y
Mol Pain, 2018, 14:1744806918777614
S8137 Capsazepine Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist.
J Ethnopharmacol, 2022, 291:115157
Int J Mol Sci, 2021, 22(11)5551
Chem Biol Interact, 2021, 351:109756
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
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. RN-1747 also antagonizes TRPM8 with IC50 of 4 μM.

E2515New JT010 JT010 is a potent agonist of transient receptor potential cation channel subfamily A member 1 (TRPA1) with an EC50 of 0.65 nM.
E2684New Icilin Icilin is an agonist of the transient receptor potential M8 (TRPM8) ion channel with an EC50 of 1.4 μM.
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.
S1990 Capsaicin(Vanilloid) Capsaicin (Qutenza, Vanilloid) is an active component of chili peppers, which are plants belonging to the genus Capsicum. Capsaici is a TRPV1 agonist with an EC50 of 0.29 μM in HEK293 cells.
Oxid Med Cell Longev, 2022, 2022:8096009
Mar Drugs, 2022, 20(6)378
Neuroscience, 2021, S0306-4522(21)00641-2
S2963 WS-12 WS-12 is a potent TRPM8 agonist with an EC50 of 39 nM.
S3605 Borneol Borneol is a bicyclic monoterpenoid compound extracted from medicinal plants such as Blumea balsamifera, and Dryobalanops aromatica. It is a TRPM8 agonist that increases ocular surface wetness.
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.
Biosci Rep, 2021, BSR20211828
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.
S4787 Methyl syringate Methyl syringate (Syringic Acid Methyl Ester), a plant phenolic compound, is a specific and selective TRPA1 agonist.
S6122 Cyclohexanecarboxamide Cyclohexanecarboxamide (Ethyl menthane carboxamide, WS3, Hexahydrobenzamide) is a cooling agent and an agonist at TRPM8 receptors (EC50 = 3.7 μM).
S9086 Dihydrocapsaicin Dihydrocapsaicin (6,7-Dihydrocapsaicin, 8-Methyl-N-vanillylnonanamide, CCRIS1589), found in pepper (C. annuum), is a potential nutriceutical.DHC is a selective TRPV1 agonist.
S2505 Rosiglitazone (BRL-49653) maleate Rosiglitazone maleate (BRL 49653), 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. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
Front Cardiovasc Med, 2021, 8:698056
S2556 Rosiglitazone (BRL 49653) Rosiglitazone (BRL 49653) 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.
Redox Biol, 2022, 50:102256
Cancer Commun (Lond), 2022, 10.1002/cac2.12332
Free Radic Biol Med, 2022, 189:42-57
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.
E0026New 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.

E2515New JT010 JT010 is a potent agonist of transient receptor potential cation channel subfamily A member 1 (TRPA1) with an EC50 of 0.65 nM.
E2684New Icilin Icilin is an agonist of the transient receptor potential M8 (TRPM8) ion channel with an EC50 of 1.4 μM.
Tags: TRP Channel inhibitor|TRP Channel agonist|TRP Channel activator|TRP Channel inducer|TRP Channel antagonist|TRP Channel signaling pathway|TRP Channel assay kit