| Identification | Back Directory | [Name]
PF-03715455 | [CAS]
1056164-52-3 | [Synonyms]
PF-03715455
PF03715455,PF 03715455
Urea, N-[1-(3-chloro-4-hydroxyphenyl)-3-(1,1-dimethylethyl)-1H-pyrazol-5-yl]-N'-[[2-[[3-[2-[(2-hydroxyethyl)thio]phenyl]-1,2,4-triazolo[4,3-a]pyridin-6-yl]thio]phenyl]methyl]- | [Molecular Formula]
C35H34ClN7O3S2 | [MDL Number]
MFCD27987916 | [MOL File]
1056164-52-3.mol | [Molecular Weight]
700.27 |
| Hazard Information | Back Directory | [Uses]
PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values 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]. | [in vivo]
PF-03715455 treatment shows that the Vss and T1/2 are 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 Vss, and T1/2 were 0.19 L/kg, 1 hour, respectively.
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| [IC 50]
p38α: 0.88 nM (IC50); p38β: 23 nM (IC50) | [References]
[1] Norman P, et al. Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92. DOI:10.1517/13543784.2015.1006358
[2] Millan DS, et al. Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease. J Med Chem. 2011 Nov 24;54(22):7797-814. DOI:10.1021/jm200677b |
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