TRP Channel

Inhibitory Selectivity

TRP Channel Products

Catalog No. Information Product Use Citations Product Validations
S6634New

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.

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.

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.

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.

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.

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).

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.

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.

S6657New

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.

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).

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.

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.

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.

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.

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.

S6838New

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.

S2650New

RN-1734

RN-1734 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.

S0174New

TRPM8 antagonist 2

TRPM8 antagonist 2 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.

S6637New

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.

S6638New

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.

S3942

Cardamonin

Cardamonin, 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.

S8137

Capsazepine

Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist.

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.

S8238

SB366791

SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist with an IC50 of 5.7 nM.

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.

S4022

Probenecid

Probenecid 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.

S6122

Cyclohexanecarboxamide

Cyclohexanecarboxamide is a cooling agent and an agonist at TRPM8 receptors (EC50 = 3.7 μM).

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.

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.

S3935

Nonivamide

Nonivamide (pelargonic acid vanillylamide, Pseudocapsaicin, Vanillyl-N-nonylamide), present in chili peppers, is commonly manufactured synthetically and used as a food additive to add pungency to seasonings, flavorings, and spice blends. Nonivamide is a agonist, which exhibits 4d-EC50 value of 5.1 mg/L in static toxicity tests.

S9086

Dihydrocapsaicin

Dihydrocapsaicin, found in pepper (C. annuum), is a potential nutriceutical.DHC is a selective TRPV1 agonist.

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.

S4787

Methyl syringate

Methyl syringate (Syringic Acid Methyl Ester), a plant phenolic compound, is a specific and selective TRPA1 agonist.

S2505

Rosiglitazone 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.

S2556

Rosiglitazone

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.

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.

Catalog No. Information Product Use Citations Product Validations
S6634New

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.

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.

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.

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.

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.

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).

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.

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.

Catalog No. Information Product Use Citations Product Validations
S6657New

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.

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).

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
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.

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.

S6838New

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.

S2650New

RN-1734

RN-1734 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.

S0174New

TRPM8 antagonist 2

TRPM8 antagonist 2 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.

S6637New

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.

S6638New

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.

S3942

Cardamonin

Cardamonin, 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.

S8137

Capsazepine

Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist.

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.

S8238

SB366791

SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist with an IC50 of 5.7 nM.

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.

Catalog No. Information Product Use Citations Product Validations
S4022

Probenecid

Probenecid 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.

S6122

Cyclohexanecarboxamide

Cyclohexanecarboxamide is a cooling agent and an agonist at TRPM8 receptors (EC50 = 3.7 μM).

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.

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.

S3935

Nonivamide

Nonivamide (pelargonic acid vanillylamide, Pseudocapsaicin, Vanillyl-N-nonylamide), present in chili peppers, is commonly manufactured synthetically and used as a food additive to add pungency to seasonings, flavorings, and spice blends. Nonivamide is a agonist, which exhibits 4d-EC50 value of 5.1 mg/L in static toxicity tests.

S9086

Dihydrocapsaicin

Dihydrocapsaicin, found in pepper (C. annuum), is a potential nutriceutical.DHC is a selective TRPV1 agonist.

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.

S4787

Methyl syringate

Methyl syringate (Syringic Acid Methyl Ester), a plant phenolic compound, is a specific and selective TRPA1 agonist.

Catalog No. Information Product Use Citations Product Validations
S2505

Rosiglitazone 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.

S2556

Rosiglitazone

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.

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.