<Suppliers Price>

PF-04856264

Names

[ CAS No. ]:
1235397-05-3

[ Name ]:
PF-04856264

[Synonym ]:
MFCD28124397

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel
Research Areas >> Neurological Disease

[Target]

IC50: 28 (human Nav1.7), 131 nM (mouse Nav1.7), 19 nM (cynomolgus monkey Nav1.7), 42 nM (dog Nav1.7)[1]


[In Vivo]

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] Dosage: 3, 30 mg/kg Administration: I.p. Result: Significantly reduced spontaneous pain behaviors in mice.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H15N5O3S2

[ Molecular Weight ]:
437.49500

[ Exact Mass ]:
437.06200

[ PSA ]:
146.52000

[ LogP ]:
5.16218

[ Storage condition ]:
2-8°C

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ Hazard Codes ]:
T

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds