For research use only. Not for therapeutic Use.
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].
| Catalog Number | I027989 |
| CAS Number | 1788063-52-4 |
| Synonyms | 5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichlorophenyl)ethyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide |
| Molecular Formula | C25H29Cl2FN2O4S |
| Purity | ≥95% |
| InChI | InChI=1S/C25H29Cl2FN2O4S/c1-15(18-9-19(26)11-20(27)10-18)30-7-5-16(6-8-30)14-34-24-13-23(28)22(12-21(24)17-3-4-17)25(31)29-35(2,32)33/h9-13,15-17H,3-8,14H2,1-2H3,(H,29,31)/t15-/m0/s1 |
| InChIKey | SXOAHIZWCZOILH-HNNXBMFYSA-N |
| SMILES | CC(C1=CC(=CC(=C1)Cl)Cl)N2CCC(CC2)COC3=CC(=C(C=C3C4CC4)C(=O)NS(=O)(=O)C)F |
| Reference | [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. |
