PF-03715455( PF03715455 )

Catalog No. M10256 CAS No. 1056164-52-3

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PF-03715455
Note

Research use only, not for human use.
Brief Description

PF-03715455 is a highly potent and selective inhibitor for p38α MAPK with IC50 of 1.6 nM.
Description

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.
In Vitro

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

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.
Synonyms

PF03715455
Pathway

MAPK/ERK Signaling
Target

p38 MAPK
Recptor

p38 MAPK
Research Area

Inflammation/Immunology
Indication

COPD

CAS Number

1056164-52-3
Formula Weight

700.273
Molecular Formula

C35H34ClN7O3S2
Purity

>98% (HPLC)
Solubility

——
SMILES

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
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

1. Millan DS, et al. J Med Chem. 2011 Nov 24;54(22):7797-814. 2. Singh D, et al. Eur J Clin Pharmacol. 2015 Oct;71(10):1175-84.

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