SB-705498
TRPV1 antagonist / Potent and selective antagonist of the TRPV1 receptor (IC50’s for receptor induction method: Capsaicin = 3 nM; Acid (pH5.3) = pIC50 7.1, and Heat = 6 nM) with activity in human, rat, and guinea pig receptors.1,2 SB-705498s activity is voltage dependent and shows >100 fold selectivity over the closely related TRPM8 receptor.2
Biochemicals & reagents
501951-42-4
Rami et al. (2006), Discovery of SB-705498: a potent and orally bioavailable TRPV1 antagonist suitable for clinical development; Bioorg. Med. Chem. Lett., 16 3287 Gunthorpe et al. (2007), Characterization of SB-705498, a Potent and Selective Vanilloid Receptor-1 (VR1/TRPV1) Antagonist That Inhibits the Capsaicin-, Acid-, and Heat-Mediated Activation of the Receptor; J. Pharmacol. Exp. Ther., 321 1183
-20°C
TARGET: Ion channel -- PATHWAY: Cation channel -- RESEARCH AREA: Neuroscience