GDC-0310 |
| Catalog No.GC64206 |
GDC-0310 es un inhibidor selectivo de Nav1.7 acil-sulfonamida, con una IC50 de 0,6 nM para hNav1.7.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1788063-52-4
Sample solution is provided at 25 µL, 10mM.
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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.
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