GNE-616 |CAS:2244895-99-4 Probechem Biochemicals

Chemical Structure : GNE-616

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GNE-616 (GNE616;GNE 616)

货号: PC-36160Not For Human Use, Lab Use Only.

GNE-616 (GNE616) is a highly potent, metabolically stable, subtype selective inhibitor of Nav1.7 with Ki of 0.79 nM (hNav1.7).

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生物&药学活性

GNE-616 (GNE616) is a highly potent, metabolically stable, subtype selective inhibitor of Nav1.7 with Ki of 0.79 nM (hNav1.7).
GNE-616 shows robust, concentration dependent reduction in nociceptive events with an EC50 of 740 nM.
GNE-616 is a highly potent inhibitor of Nav1.7 in manual patch clamp electrophysiology assays (Kd=0.38 nM), showing >1000-fold selectivity over Nav1.1, Nav1.3, Nav1.4, and Nav1.5 and modest selectivity over Nav1.2 and Nav1.6 (30-70 fold).
GNE-616 shows a robust PK/PD response in a Nav1.7 dependent mouse model.

物理化学性质&存储条件

分子量	537.534
分子式	C24H23F4N5O3S
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
Chemical Name/SMILES	(S)-6-fluoro-4-((2R,4S)-2-(pyridin-2-yl)-4-(trifluoromethyl)piperidin-1-yl)-N-(pyrimidin-4-yl)chromane-7-sulfonamide

参考文献

1. McKerrall SJ, et al. J Med Chem. 2019 Apr 3. doi: 10.1021/acs.jmedchem.9b00141.

GNE-616 (GNE616;GNE 616)

生物&药学活性

物理化学性质&存储条件

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GNE-616 (GNE616;GNE 616)

生物&药学活性

物理化学性质&存储条件

参考文献

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