PF-03715455

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-03715455 是一种高效、选择性的 p38α MAPK 抑制剂，IC50 为 1.6 nM。

PF-03715455 is a highly potent and selective inhibitor for p38α MAPK with IC50 of 1.6 nM; shows efficacy and safety profiles as an inhaled agent for the treatment of COPD.COPD Phase 2 Discontinued.

PF-03715455 is a moderate inhibitor of CYP1A2, CYP2C19, and CYP2D6 and a potent inhibitor of CYP’s 2C9 and CYP3A4.

PF-03715455 treatment shows that the Vss and T1/2 are 0.19 L/kg, 1 hour, respectively. Animal Model:Male CD Sprague Dawley rats (300-450 g)Dosage:1 mg/kg Administration:I.v. (Pharmacokinetic Analysis)Result:The Vss, and T1/2 were 0.19 L/kg, 1 hour, respectively.

PF03715455

MAPK/ERK Signaling

p38 MAPK

p38 MAPK

Inflammation/Immunology

COPD

1056164-52-3

700.273

C35H34ClN7O3S2

>98% (HPLC)

——

CC(C)(C)C1=NN(C(=C1)NC(=O)NCC2=CC=CC=C2SC3=CN4C(=NN=C4C5=CC=CC=C5SCCO)C=C3)C6=CC(=C(C=C6)O)Cl

1-(3-(tert-butyl)-1-(3-chloro-4-hydroxyphenyl)-1H-pyrazol-5-yl)-3-(2-((3-(2-((2-hydroxyethyl)thio)phenyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl)thio)benzyl)urea

(-20℃)

With Ice Pack

≥ 2 years