1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. PF-04856264

PF-04856264 

Cat. No.: HY-12811
Handling Instructions

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.

For research use only. We do not sell to patients.

PF-04856264 Chemical Structure

PF-04856264 Chemical Structure

CAS No. : 1235397-05-3

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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].

IC50 & 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.
Molecular Weight

437.49

Formula

C₂₀H₁₅N₅O₃S₂

CAS No.

1235397-05-3

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PF-04856264PF04856264PF 04856264Sodium ChannelNa channelsNa+ channelssubtypeselectivechannelanalgesicspontaneouspainInhibitorinhibitorinhibit

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PF-04856264
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HY-12811
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