189512

Inhibitor autotaksyny III, PF-8380

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.

• Synonim(y): 6-(3-(piperazyn-1-ylo)propanoilo)-benzo[d]oksazol-2(3H)-on, Atx Inhibitor III, PF-8380
• Wzór empiryczny (zapis Hilla): C₂₂H₂₁Cl₂N₃O₅
• Numer CAS: 1144035-53-9
• Masa cząsteczkowa: 478.33
• UNSPSC Code: 51111800
• NACRES: NA.28
• MDL number: MFCD20527274
• Assay: ≥95% (HPLC)
• Form: powder
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Właściwości

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: tan
• solubility: DMSO: 100 mg/mL
• shipped in: dry ice
• storage temp.: −20°C
• SMILES string: O=C(OCC1=CC(Cl)=CC(Cl)=C1)N2CCN(CCC(C3=CC(OC(N4)=O)=C4C=C3)=O)CC2
• InChI: 1S/C22H21Cl2N3O5/c23-16-9-14(10-17(24)12-16)13-31-22(30)27-7-5-26(6-8-27)4-3-19(28)15-1-2-18-20(11-15)32-21(29)25-18/h1-2,9-12H,3-8,13H2,(H,25,29)
• InChI key: JMSUDQYHPSNBSN-UHFFFAOYSA-N

Opis

General 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-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.).

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable