PF-04856264是一种有效选择性的Nav1.7抑制剂，人、小鼠、食蟹猴和狗Nav1.7的IC50分别为28、131、19和42nM。PF-04856264对大鼠Nav1.7通道的抑制作用较弱。PF-04856264有镇痛作用。
货号:ajcx31278
CAS:1235397-05-3
分子式:C20H15N5O3S2
分子量：437.49
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect[1][2].

PF-04856264 (3-30 mg/kg; i.p.) reverses OD1-induced pain behaviors[2]. Animal Model: 6-8 weeks adult male C57BL/6J mice (OD1-induced spontaneous pain model)[2]

[1]. McCormack K, et al. Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels. Proc Natl Acad Sci U S A. 2013;110(29):E2724-E2732. [2]. Deuis JR, et al. Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain. Toxins (Basel). 2016;8(3):78. Published 2016 Mar 17.