Autotaxin Inhibitor III, PF-8380-CAS 1144035-53-9-Calbiochem

C₂₂H₂₁Cl₂N₃O₅

478.33

MFCD20527274

An orally bioavailable piperazinylbenzoxazolone compound that acts as a substrate competitive and tight-binding inhibitor of autotaxin activity {IC₅₀ = 2.8 and 1.7 nM for recombinant human enzyme-β isoform employing FS-3 and LPC (lysophosphatidylcholine) as substrates, respectively; 1.16 and 1.15 nM for rat/murine enzyme-FS-3 and fetal fibroblast cell-LPC; 101 nM for human whole blood}. Displays desirable pharmacokinetics properties and efficiently blocks inflammation-induced LPA (lysophosphatidic acid) production both in plasma and at the site of inflammation by 95% in rat adjuvant-induced arthritis model (30 mg/kg, p.o.).

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Gierse, J., et al. 2010. J. Pharmacol. Exp. Ther.334, 310.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥95% (HPLC)

powder

Calbiochem^®

OK to freeze
protect from light

tan

DMSO: 100 mg/mL

dry ice

−20℃

O=C(OCC1=CC(Cl)=CC(Cl)=C1)N2CCN(CCC(C3=CC(OC(N4)=O)=C4C=C3)=O)CC2

10 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 3