Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 4-[3-(2,3-dihydro-2-oxo-6-benzoxazolyl)-3-oxopropyl]-(3,5-dichlorophenyl)methyl ester-1-piperazinecarboxylic acid
Purity: ≥95%
Formula Markup: C22H21Cl2N3O5
Formula Weight: 478.3
CAS Number: 1144035-53-9
Notes: Autotaxin converts lysophosphatidylcholine to lysophosphatidic acid (LPA), which can mediate changes in cell proliferation, angiogenesis, and cytokine secretion.{21340} 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).{21340} It reverses MMP-13 expression induced by leptin in human OA chondrocytes when used at a concentration of 10 µM.{35249} 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).{21340}
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