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PZ0236 Sigma-Aldrich

CP-863187

≥98% (HPLC)

Synonym: 4-(2,5-Difluorophenyl)-5-(3-isopropyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxazole, 6-[4-(2,5-Difluorophenyl)-5-oxazolyl]-3-(1-methylethyl)-1,2,4-triazolo[4,3-a]pyridine, 6-[4-(2,5-Difluorophenyl)oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine, CP863187

  • CAS Number 668981-02-0

  • Empirical Formula (Hill Notation) C18H14F2N4O

  • Molecular Weight 340.33

  •  MDL number MFCD30480740

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, CI-CZ, Cell Biology, Cell Signaling and Neuroscience,
Quality Level   100
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 10 mg/mL, clear
storage temp.   room temp
SMILES string   FC1=C(C2=C(OC=N2)C(C=C3)=CN4C3=NN=C4C(C)C)C=C(F)C=C1

Description

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

CP-863187 is a potent p38α (p38α) inhibitor (IC50 = 5.8 nM) with 44-fold selectivity over p38β (p38β) and no inhibitory potency against p38γ (p38γ) and p38δ (p38δ) isoforms. CP-863187 effectively inhibits LPS-stimulated cellular TNF-α production in vitro (IC50 = 259 and 25 nM, using human whole blood and isolated mononuclear cells, respectively) and in rats in vivo (ED50 = 0.3 mg/kg p.o.) with good pharmacokinetic profile and oral availability (F = 87%/dog, 40%/monkey, 30%/rat with 5 mg/kg oral dosage; F = 66%/rat with 50 mg/kg oral dosage).

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles

Articles

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