PF-04856264

Modify Date: 2024-07-23 01:51:23

PF-04856264 Structure
PF-04856264 structure
Common Name PF-04856264
CAS Number 1235397-05-3 Molecular Weight 437.49500
Density N/A Boiling Point N/A
Molecular Formula C20H15N5O3S2 Melting Point N/A
MSDS Chinese USA Flash Point N/A
Symbol GHS06
GHS06
Signal Word Danger

 Use of 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].

 Names

Name 3-cyano-4-(2-(1-methyl-1H-pyrazol-5-yl)phenoxy)-N-(thiazol-2-yl)benzenesulfonamide
Synonym More Synonyms

 PF-04856264 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
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
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
Hazard Codes T
RIDADR UN 2811 6.1 / PGIII

 Synonyms

MFCD28124397
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