| Identification | Back Directory | [Name]
3-Cyano-4-[2-(1-methyl-1H-pyrazol-5-yl)phenoxy]-N-2-thiazolyl-benzenesulfonamide | [CAS]
1235397-05-3 | [Synonyms]
PF4856264
PF-4856264
PF 4856264
PF-04856264
PF 04856264,PF04856264
PF-04856264 >=98% (HPLC)
3-Cyano-4-[2-(1-methyl-1H-pyrazol-5-yl)phenoxy]-N-2-thiazolyl-benzenesulfonamide
3-cyano-4-[2-(2-methylpyrazol-3-yl)phenoxy]-N-(1,3-thiazol-2-yl)benzenesulfonamide
Benzenesulfonamide, 3-cyano-4-[2-(1-methyl-1H-pyrazol-5-yl)phenoxy]-N-2-thiazolyl-
3-CYANO-4-(2-(1-METHYL-1H-PYRAZOL-5-YL) PHENOXY)-N-(THIAZOL-2-YL) BENZENESULFONAMIDE | [Molecular Formula]
C20H15N5O3S2 | [MDL Number]
MFCD28124397 | [MOL File]
1235397-05-3.mol | [Molecular Weight]
437.49 |
| Chemical Properties | Back Directory | [Boiling point ]
635.0±65.0 °C(Predicted) | [density ]
1.44±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble10mg/mL, clear | [form ]
powder | [pka]
5.68±0.10(Predicted) | [color ]
white to light brown |
| Hazard Information | Back Directory | [Uses]
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]. | [Biochem/physiol Actions]
PF-04856264 is a potent, selective inhibitor of the human Nav1.7 voltage gated sodium channel (IC50 = 28 nM). PF-04856264 blocks mouse Nav1.7 (IC50 = 131 nM) but has low potency against the rat Nav1.7 channel (IC50 = 4.2 mM). | [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.
|
| [IC 50]
Nav1.7 | [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. DOI:10.1073/pnas.1220844110
[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. DOI:10.3390/toxins8030078 |
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