PF-03715455|PF03715455|CAS 1056164-52-3|DC Chemicals

Cas No.:	1056164-52-3
Chemical Name:	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
Synonyms:	PF03715455;PF-03715455;PF 03715455
SMILES:	O=C(NC1N(C2C=C(Cl)C(O)=CC=2)N=C(C(C)(C)C)C=1)NCC1C(SC2C=CC3=NN=C(C4C(SCCO)=CC=CC=4)N3C=2)=CC=CC=1
Formula:	C₃₅H₃₄ClN₇O₃S₂
M.Wt:	700.27
Purity:	>97%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[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.

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].
Target:	p38α:0.88 nM (IC50) p38β:23 nM (IC50)
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.
In Vitro:	PF-03715455 is a moderate inhibitor of CYP1A2, CYP2C19, and CYP2D6 and a potent inhibitor of CYP’s 2C9 and CYP3A4[2].
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.

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