|S2773||SB705498||<1 mg/mL||86 mg/mL||20 mg/mL|
|S4022||Probenecid||<1 mg/mL||57 mg/mL||22 mg/mL|
|S7115||AMG-517||<1 mg/mL||86 mg/mL||<1 mg/mL|
|S8137||Capsazepine||<1 mg/mL||75 mg/mL||75 mg/mL|
|S3605||Borneol||<1 mg/mL||30 mg/mL||30 mg/mL|
|S8367||GSK2193874||<1 mg/mL||100 mg/mL||50 mg/mL|
|S8107||GSK1016790A||<1 mg/mL||100 mg/mL||100 mg/mL|
|S8238||SB366791||<1 mg/mL||57 mg/mL||<1 mg/mL|
|S4516||(+)-Camphor||<1 mg/mL||30 mg/mL||30 mg/mL|
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.
(B) SK-N-SH cells were incubated with AM251 (CB1 antagonist) or SB705498 (TRPV-1 antagonist) for 30 min and stimulated with NADA (10 μM) for 6 h. The expression of HIF-1α protein was determined by immunoblot analysis. We show a representative blot of three independent experiments.
Probenecid is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16.
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.
Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist.
Methyl salicylate is an organic ester naturally produced by many species of plants, particularly wintergreens. It is an agonist for TRPA1 and TRPV1.
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.
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.
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.
GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.
SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist.
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.