PF-05089771

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-05089771 是一种有效的、状态依赖性、亚型选择性 Nav1.7 抑制剂，IC50 为 11 nM。

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; 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); displays high selectivity over L-type calcium channels, KvLQT and hERG potassium channels; demonstrates in vivo efficacy in a mouse capsaicin-induced neurogenic flare model.

PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Nav1.5 and Nav1.8 channels (IC50s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Nav1.2 to 900-fold for Nav1.3 and Nav1.4).PF-05089771 (30 nM) blocks the majority of TTX-S current (75.5 ± 10.5%, n = 5) whilst 100 nM resulted in complete block.

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PF05089771

Membrane Transporter/Ion Channel

Sodium Channel

Na(V1.7) channel

Neurological Disease

Pain

1430806-04-4

500.344

C18H12Cl2FN5O3S2

>98% (HPLC)

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CC1=CC=C(C=C1)S(=O)(=O)O.C1=CC(=C(C=C1Cl)C2=C(NN=C2)N)OC3=CC(=C(C=C3Cl)S(=O)(=O)NC4=CSC=N4)F

4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years