PF-8380

Autotaxin converts lysophosphatidylcholine to lysophosphatidic acid (LPA), which can mediate changes in cell proliferation, angiogenesis, and cytokine secretion. PF-8380 is a potent inhibitor of autotaxin (IC50 = 2.8 nM in an enzyme assay), the enzyme that converts lysophosphatidylcholine to lysophosphatidic acid (LPA). It reverses MMP-13 expression induced by leptin in human OA chondrocytes when used at a concentration of 10 µM. PF-8380 (30 mg/kg) reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).Formal Name: 4-[3-(2,3-dihydro-2-oxo-6-benzoxazolyl)-3-oxopropyl]-(3,5-dichlorophenyl)methyl ester-1-piperazinecarboxylic acid. CAS Number: 1144035-53-9. Molecular Formula: C22H21Cl2N3O5. Formula Weight: 478.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS(pH 7.2)(1:6): 0.14 mg/ml, DMSO: 3 mg/ml. lambdamax: 220, 273, 292 nm. SMILES: O=C(C1=CC(OC(N2)=O)=C2C=C1)CCN3CCN(C(OCC4=CC(Cl)=CC(Cl)=C4)=O)CC3. InChi Code: 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.