PF-03715455

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PF-03715455

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1056164-52-3

PF-03715455 是一种有效的吸入的p38 MAPK抑制剂，对 p38α 有一定的选择性，对 p38α 和 p38β 的IC₅₀值分别为 0.88 和 23 nM。PF-03715455 对 LPS 诱导的人全血 TNFα 产生有抑制作用 (IC₅₀=1.7 nM)。PF-03715455 有用于慢性阻塞性肺病 (COPD) 的潜力。

生物活性

PF-03715455 is a potent inhaledp38 MAPKinhibitor. PF-03715455 shows some selectivity forp38αoverp38βwith respectiveIC₅₀values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC₅₀=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease)^[1]^[2].

IC₅₀& Target^[1]

p38α

0.88 nM (IC₅₀)

p38β

23 nM (IC₅₀)

体外研究
(In Vitro)

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

体内研究
(In Vivo)

PF-03715455 treatment shows that the V_ssand T_1/2are 0.19 L/kg, 1 hour, respectively^[2].

Animal Model:	Male CD Sprague Dawley rats (300-450 g)^[2]
Dosage:	1 mg/kg
Administration:	I.v. (Pharmacokinetic Analysis)
Result:	The V_ss, and T_1/2were 0.19 L/kg, 1 hour, respectively.

Clinical Trial

分子量

700.27

Formula

C₃₅H₃₄ClN₇O₃S₂

CAS 号

1056164-52-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.