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PZ0236

Sigma-Aldrich

CP-863187

≥98% (HPLC)

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C18H14F2N4O
CAS Number:
668981-02-0
Molecular Weight:
340.33
MDL number:
MFCD30480740
UNSPSC Code:
12352200

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

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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