TRP Channel

Inhibitory Selectivity

TRP Channel Products

New TRP Channel Products
Catalog No. Information Product Use Citations Product Validations
S2918

HC-030031

HC-030031 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.

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.

S6410New

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.

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.

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.

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.

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.

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.

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 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

Cardamonin 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.

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.

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, a plant phenolic compound, is a specific and selective TRPA1 agonist.

S6409New

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
S2918

HC-030031

HC-030031 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.

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.

S6410New

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.

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.

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.

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.

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.

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.

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 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

Cardamonin 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.

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.

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, a plant phenolic compound, is a specific and selective TRPA1 agonist.

Catalog No. Information Product Use Citations Product Validations
S6409New

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.