1788063-52-4

1788063-52-4 structure

Name: GDC-0310
Chemical Name: (S) -methyl 5-cyclopropyl-4- ( (1- (1- (3, 5-dichlorophenyl) ethyl) piperidin-4-yl) methoxy) -2-fluorobenzoate
CAS Number: 1788063-52-4
Molecular Formula: C₂₅H₂₈Cl₂FNO₃
Molecular Weight: 480.3991232
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
Create Date: 2018-07-02 02:00:42
Modify Date: 2024-01-02 19:26:12
GDC-0310 is a selective acyl-sulfonamide Nav1.7 inhibitor, with an IC50 of 0.6 nM for hNav1.7[1].

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

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.

Molecular Formula	C₂₅H₂₈Cl₂FNO₃
Molecular Weight	480.3991232