GDC-0310 是选择性的 Nav1.7 酰磺酰胺抑制剂，其对 hNav1.7 的 IC50 值为 0.6 nM。
货号:ajcx37168
CAS:1788063-52-4
分子式:C25H29Cl2FN2O4S
分子量：543.48
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

GDC-0310 is a selective acyl-sulfonamide Nav1.7 inhibitor, with an IC50 of 0.6 nM for hNav1.7[1].

GDC-0310 exhibits an EC50 of 1.1 μM in vivo and a Ki of 1.8 nM for Nav1.7[1].

GDC-0310 shows substantially improved Nav selectivity and ADME properties[1].GDC-0310 exhibits t1/2 values of 5 h, 46 h and 4.4 h in rat (5 mg/kg, iv), dog (1 mg/kg, iv) and cynomolgus monkeys (2 mg/kg, iv), respectively[1].

[1]. Brian S Safina, et al. Discovery of Acyl-sulfonamide Na v 1.7 Inhibitors GDC-0276 and GDC-0310. J Med Chem. 2021 Mar 25;64(6):2953-2966.
[2]. Lei Xu, et al. Voltage-gated sodium channels: structures, functions, and molecular modeling. Drug Discov Today. 2019 Jul;24(7):1389-1397.