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GSK1014802 Raxatrigine

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产品信息

产品名称：GSK1014802 Raxatrigine	纯度：98% min
CAS NO：934240-30-9	溶解度：DMSO : 83 mg/mL (264.04 mM)
分子式：C₁₈H₁₉FN₂O₂	包装：可按客户要求包装
分子量：314.354	贮存：-20℃

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备注说明

Raxatrigine (GSK-1014802) 是钠离子通道Nav1.7有效抑制剂。

Raxatrigine, also known as GSK1014802 and CNV-1014802, is a sodium channel antagonist that is currently in phase II studies in bipolar depression. CNV1014802 is a peripherally and centrally acting agent that inhibits sodium channels in a state-dependent fashion. CNV1014802 shows selectivity for the Nav1.7 subtype over the other subtypes tested (Nav1.1, Nav1.2, Nav1.3, Nav1.5, Nav1.6 and TTX-R), for both the resting and depolarized states.

参考文献

[1]. Large CH, et al. The efficacy of sodium channel blockers to prevent phencyclidine-induced cognitive dysfunction in the rat: potential for novel treatments for schizophrenia. J Pharmacol Exp Ther. 2011 Jul;338(1):100-13.