PF-04856264

Names

[ 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

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.