| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 28 (human Nav1.7), 131 nM (mouse Nav1.7), 19 nM (cynomolgus monkey Nav1.7), 42 nM (dog Nav1.7) | ||||||||||||
| In Vivo | PF-04856264 (3-30 mg/kg; i.p.) reverses OD1-induced pain behaviors[2]. Animal Model: | ||||||||||||
| Name | PF-04856264 | ||||||||||||
| CAS | 1235397-05-3 | ||||||||||||
| Formula | C20H15N5O3S2 | ||||||||||||
| Molar Mass | 437.49 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
PF-04856264
CAS: 1235397-05-3 F: C20H15N5O3S2 W: 437.49
PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgu
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