PF-05089771 free base

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PF-05089771 free base 是一种有效的亚型选择性 Nav1.7 抑制剂，IC50 为 11 nM。

PF-05089771 free base is a potent, subtype selective Nav1.7 inhibitor with IC50 of 11 nM, shows no activity against Nav 1.5 and >10-fold selectivity over other Nav isoforms; specifically interacts with the voltage-sensor domain (VSD4); blocks the majority of TTX-S current (75%) at 30 nM in human DRG neurons (IC50=8.4 nM); exhibits action potentials in spinal slice electrophysiology recordings, mouse and human DRG neurons, demonstrates in vivo efficacy 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, Fig 5D) whilst 100 nM resulted in complete block.

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PF05089771 free base

Membrane Transporter/Ion Channel

Sodium Channel

Sodium Channel

Neurological Disease

Pain

1235403-62-9

500.354

C18H12Cl2FN5O3S2

>98% (HPLC)

DMSO: ≥ 34 mg/mL

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

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

(-20℃)

With Ice Pack

≥ 2 years