PF-04856264 |
| カタログ番号GC61174 |
PF-04856264 は、強力かつ選択的な Nav1.7 阻害剤であり、IC50 は、ヒト、マウス、カニクイザル、およびイヌ Nav1.7 に対してそれぞれ 28、131、19、および 42 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1235397-05-3
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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