PZ0236

CP-863187

≥98% (HPLC)

• Synonym(e): 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
• Empirische Formel (Hill-System): C₁₈H₁₄F₂N₄O
• CAS-Nummer: 668981-02-0
• Molekulargewicht: 340.33
• MDL-Nummer: MFCD30480740
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 10 mg/mL, clear
• Lagertemp.: room temp
• SMILES String: FC1=C(C2=C(OC=N2)C(C=C3)=CN4C3=NN=C4C(C)C)C=C(F)C=C1

Beschreibung

Biochem./physiol. Wirkung

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).

Rechtliche Hinweise

Sold for research purposes under agreement from Pfizer Inc.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable