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Autotaxin Inhibitor III, PF-8380 - CAS 1144035-53-9 - Calbiochem The Autotaxin Inhibitor III, PF-8380, also referenced under CAS 1144035-53-9, controls the biological activity of Autotaxin. This small molecule/inhibitor is primarily used for Membrane applications.

Item no.

SAF-189512-10MG

Unit

1 x 10 mg

Shipment details

No Dangerous Good

Price on request

Description

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-beta 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.).

Structure formula

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