PF-05089771 | Nav1.7 inhibitor | Probechem Biochemicals

Chemical Structure : PF-05089771

CAS No.: 1235403-62-9

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PF-05089771 (PF05089771)

货号: PC-63166Not For Human Use, Lab Use Only.

PF-05089771 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 11 nM, >1,000-fold selectivity over Nav1.3, 1.4 and Nav1.5, 1.8.

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10 mg	￥2580	In stock
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生物&药学活性

PF-05089771 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 11 nM, >1,000-fold selectivity over Nav1.3, 1.4 and Nav1.5, 1.8.
PF-05089771 interacts with the voltage-sensor domain (VSD) of domain IV, blocks all Nav1.7 splice variants with similar potency (5N11L, 5A11S, 5A11L and 5N11S, IC50s=11=33 nM).
PF-05089771 displays high selectivity over L-type calcium channels, KvLQT and hERG potassium channels.
PF-05089771 demonstrates in vivo efficacy in a mouse capsaicin-induced neurogenic flare model.

物理化学性质&存储条件

分子量	500.344
分子式	C18H12Cl2FN5O3S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide

参考文献

1. Swain NA, et al. J Med Chem. 2017 Aug 24;60(16):7029-7042.

2. Theile JW, et al. Mol Pharmacol. 2016 Nov;90(5):540-548.

3. Alexandrou AJ, et al. PLoS One. 2016 Apr 6;11(4):e0152405.

4. Chernov-Rogan T, et al. Proc Natl Acad Sci U S A. 2018 Jan 23;115(4):E792-E801.

PF-05089771 (PF05089771)

生物&药学活性

物理化学性质&存储条件

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PF-05089771 (PF05089771)

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