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GNE-616

Names

[ CAS No. ]:
2244895-99-4

[ Name ]:
GNE-616

Biological Activity

[Description]:

GNE-616 (GNE616) is a highly potent, metabolically stable, subtype selective inhibitor of Nav1.7 with Ki of 0.79 nM (hNav1.7); 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); shows a robust PK/PD response in a Nav1.7 dependent mouse model.

[References]

References 1. McKerrall SJ, et al. J Med Chem. 2019 Apr 3. doi: 10.1021/acs.jmedchem.9b00141. View Related Products by Target Sodium Channel

Chemical & Physical Properties

[ Molecular Formula ]:
C24H23F4N5O3S

[ Molecular Weight ]:
537.534


Related Compounds