AS1928370

AS1928370 (ASP8370) is a potent, selective, orally available TRPV1 antagonist with IC50 of 0.51 uM, shows no inhibitory effects on TRPV4, TRPA11, and TRPM8 at 10 uM; demonstrates high aqueous solubility (pH6.8, >100 uM), satisfactory stability in human liver microsomes, and reduced CYP3A4 inhibition; improves capsaicin-induced secondary hyperalgesia and mechanical allodynia in an L5/L6 spinal nerve ligation model in rats with respective ED50s of 0.17 and 0.26 mg/kg p.o.

References 1. Oka H, et al. Bioorg Med Chem. 2018 Jul 23;26(12):3716-3726. 2. Watabiki T, et al. J Pharmacol Exp Ther. 2011 Mar;336(3):743-50. 3. Watabiki T, et al. Biol Pharm Bull. 2011;34(7):1105-8. View Related Products by Target TRP Channel