3-Cyano-4-[2-(1-methyl-1H-pyrazol-5-yl)phenoxy]-N-2-thiazolyl-benzenesulfonamide
- Product Name
- 3-Cyano-4-[2-(1-methyl-1H-pyrazol-5-yl)phenoxy]-N-2-thiazolyl-benzenesulfonamide
- CAS No.
- 1235397-05-3
- Chemical Name
- 3-Cyano-4-[2-(1-methyl-1H-pyrazol-5-yl)phenoxy]-N-2-thiazolyl-benzenesulfonamide
- 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;Benzenesulfonamide, 3-cyano-4-[2-(1-methyl-1H-pyrazol-5-yl)phenoxy]-N-2-thiazolyl-;3-cyano-4-[2-(2-methylpyrazol-3-yl)phenoxy]-N-(1,3-thiazol-2-yl)benzenesulfonamide;3-CYANO-4-(2-(1-METHYL-1H-PYRAZOL-5-YL) PHENOXY)-N-(THIAZOL-2-YL) BENZENESULFONAMIDE
- CBNumber
- CB52750715
- Molecular Formula
- C20H15N5O3S2
- Formula Weight
- 437.49
- MOL File
- 1235397-05-3.mol
3-Cyano-4-[2-(1-methyl-1H-pyrazol-5-yl)phenoxy]-N-2-thiazolyl-benzenesulfonamide Property
- 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
- pka
- 5.68±0.10(Predicted)
- form
- powder
- color
- white to light brown
N-Bromosuccinimide Price
- Product number
- SML1061
- Product name
- PF-04856264
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $137
- Updated
- 2025/07/31
- Product number
- SML1061
- Product name
- PF-04856264
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $546
- Updated
- 2025/07/31
- Product number
- CS-0012528
- Product name
- PF-04856264
- Purity
- ≥99.0%
- Packaging
- 5mg
- Price
- $504
- Updated
- 2021/12/16
- Product number
- CM331018
- Product name
- 3-cyano-4-[2-(2-methylpyrazol-3-yl)phenoxy]-N-(1,3-thiazol-2-yl)benzenesulfonamide
- Purity
- 95%+
- Packaging
- 100mg
- Price
- $582
- Updated
- 2021/12/16
- Product number
- CM331018
- Product name
- 3-cyano-4-[2-(2-methylpyrazol-3-yl)phenoxy]-N-(1,3-thiazol-2-yl)benzenesulfonamide
- Purity
- 95%+
- Packaging
- 250mg
- Price
- $965
- Updated
- 2021/12/16
3-Cyano-4-[2-(1-methyl-1H-pyrazol-5-yl)phenoxy]-N-2-thiazolyl-benzenesulfonamide Chemical Properties,Usage,Production
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
3-Cyano-4-[2-(1-methyl-1H-pyrazol-5-yl)phenoxy]-N-2-thiazolyl-benzenesulfonamide Preparation Products And Raw materials
Raw materials
Preparation Products
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