85-2071-56 [受注停止]Autotaxin Inhibitor III, PF-8380 (Atx Inhibitor III, PF-8380, 6-(3-(Piperazin-1-yl)propanoyl)-benzo[d]oxazol-2(3H)-one) 10mg CAS No:1144035-53-9 217206
An orally bioavailable piperazinylbenzoxazolone compound that acts as a substrate competitive and tight-binding inhibitor of autotaxin activity {IC50=2.8 and 1.7nM for recombinant human enzyme-b isoform employing FS-3 and LPC (lysophosphatidylcholine) as substrates, respectively; 1.16 and 1.15nM for rat/murine enzyme-FS-3 and fetal fibroblast cell-LPC; 101nM 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 (30mg/kg, p.o.).
Synonyms:6-(3-(Piperazin-1-yl)propanoyl)-benzo[d]oxazol-2(3H)-one, Atx Inhibitor III, PF-8380
Molecular Formula:C₂₂H₂₁Cl₂N₃O₅
Solubility:DMSO
Molecular Weight:478.3
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Important Note:This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Toxicity and Hazards: All products should be handled by qualified personnel only, trained in laboratory procedures.