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Chemical Structure : GNE-616
Catalog No.: 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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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.
| M.Wt | 537.534 | |
| Formula | C24H23F4N5O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. McKerrall SJ, et al. J Med Chem. 2019 Apr 3. doi: 10.1021/acs.jmedchem.9b00141.
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