|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|
|S8367||GSK2193874||<1 mg/mL||100 mg/mL||50 mg/mL|
|S3605||Borneol||<1 mg/mL||30 mg/mL||30 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.
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.
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.
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.