PF-03715455

Modify Date: 2024-04-06 09:22:50

PF-03715455 Structure
PF-03715455 structure
Common Name PF-03715455
CAS Number 1056164-52-3 Molecular Weight 700.27300
Density N/A Boiling Point N/A
Molecular Formula C35H34ClN7O3S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PF-03715455


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].

 Names

Name 1-[5-tert-butyl-2-(3-chloro-4-hydroxyphenyl)pyrazol-3-yl]-3-[[2-[[3-[2-(2-hydroxyethylsulfanyl)phenyl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]sulfanyl]phenyl]methyl]urea
Synonym More Synonyms

 PF-03715455 Biological Activity

Description 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].
Related Catalog
Target

p38α:0.88 nM (IC50)

p38β:23 nM (IC50)

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

[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.

 Chemical & Physical Properties

Molecular Formula C35H34ClN7O3S2
Molecular Weight 700.27300
Exact Mass 699.18500
PSA 183.69000
LogP 8.07320

 Synonyms

2yis
UNII-0TJ631J0KP
PF-03715455
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