GDC-0310

Modify Date: 2024-01-02 19:26:12

GDC-0310 Structure
GDC-0310 structure
Common Name GDC-0310
CAS Number 1788063-52-4 Molecular Weight 480.3991232
Density N/A Boiling Point N/A
Molecular Formula C25H28Cl2FNO3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GDC-0310


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

 Names

Name (S) -methyl 5-cyclopropyl-4- ( (1- (1- (3, 5-dichlorophenyl) ethyl) piperidin-4-yl) methoxy) -2-fluorobenzoate

 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
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
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