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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-GDC-0276
GDC-0276

Chemical Structure : GDC-0276

CAS No.: 1494581-70-2

GDC-0276 (GDC 0276)

货号: PC-72192Not For Human Use, Lab Use Only.

GDC-0276 (GDC 0276) is a highly potent, selective NaV1.7 inhibitor with IC50 of with binding Ki of 1.1 nM (hNaV1.7), cellular sodium influx IC50 of 49 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GDC-0276 (GDC 0276) is a highly potent, selective NaV1.7 inhibitor with IC50 of with binding Ki of 1.1 nM (hNaV1.7), cellular sodium influx IC50 of 49 nM.
GDC-0276 displays 18-fold selectivity over NaV1.5 (cellular sodium influx IC50=870 nM), as well as 26-1200-fold selectivity over NaV1.1/1.2/1.6 (potency measured by voltage clamp).
GDC-0276 showed a concentration dependent reduction in nociceptive events, with a EC50 of 1.7 μM in inherited erythromelalgia (IEM) mouse model.

物理化学性质&存储条件

分子量 462.58
分子式 C24H31FN2O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO (4.6 mg/mL)

Chemical Name/SMILES

4-((Adamantan-1-yl)methoxy)-N-(azetidin-1-ylsulfonyl)-5-cyclopropyl-2-fluorobenzamide

参考文献

1. Brian S Safina, et al. J Med Chem. 2021 Mar 25;64(6):2953-2966.

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