PF-04856264

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].

Product Specifications

CAS Number

[1235397-05-3]

UNSPSC

12352005

Hazard Statement

H301

Target

Sodium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/pf-04856264.html

Concentration

10mM

Purity

99.29

Solubility

DMSO : 250 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=S(C1=CC=C(OC2=CC=CC=C2C3=CC=NN3C)C(C#N)=C1)(NC4=NC=CS4)=O

Molecular Formula

C20H15N5O3S2

Molecular Weight

437.49

Precautions

H301

References & Citations

[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.