Chemical Structure : AMG 8379
货号: PC-60629Not For Human Use, Lab Use Only.
AMG 8379 (AMG-8379, AMG8379) is a potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM.
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AMG 8379 (AMG-8379, AMG8379) is a potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM.
AMG 8379 potently blocks endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglion (DRG) neurons with IC50 of 3.1 nM in whole-cell patch clamp electrophysiology assays.
AMG 8379 displays100- to 1000-fold selectivity over other NaV family members, including NaV1.4 and NaV1.5.
AMG 8379 blocks mechanically induced action potential firing in C-fibers, reduces the frequency of thermally induced C-fiber spiking.
AMG 8379 exhibits pharmacodynamic effects in translatable models of both itch and pain.
分子量 | 543.926 | |
分子式 | C25H16ClF2N3O5S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Kornecook TJ, et al. J Pharmacol Exp Ther. 2017 Jul;362(1):146-160.
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