GDC-0310

Names

[ CAS No. ]:
1788063-52-4

[ Name ]:
GDC-0310

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Research Areas >> Neurological Disease

[Target]

hNav1.4:3.4 nM (IC50)

hNav1.2:38 nM (IC50)

hNav1.6:198 nM (IC50)

hNav1.1:202 nM (IC50)

hNav1.5:551 nM (IC50)

[In Vitro]

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

[In Vivo]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₈Cl₂FNO₃

[ Molecular Weight ]:
480.3991232

GDC-0310

Names

Biological Activity

Chemical & Physical Properties

Related Compounds