GDC-0310 

GDC-0310 is a selective acyl-sulfonamide Na_v1.7 inhibitor, with an IC₅₀ of 0.6 nM for hNa_v1.7^[1].

GDC-0310 exhibits an EC₅₀ of 1.1 μM in vivo and a K_i of 1.8 nM for Na_v1.7^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GDC-0310 shows substantially improved Na_v 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

543.48

C₂₅H₂₉Cl₂FN₂O₄S

1788063-52-4

Solid

White to off-white

O=C(NS(=O)(C)=O)C1=CC(C2CC2)=C(OCC3CCN([C@H](C4=CC(Cl)=CC(Cl)=C4)C)CC3)C=C1F

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]

  [2]. Lei Xu, et al. Voltage-gated sodium channels: structures, functions, and molecular modeling. Drug Discov Today. 2019 Jul;24(7):1389-1397.  [Content Brief]