Chemical Name: 3,5-Dichlorobenzyl-[4-[3-oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]]piperazine-1-carboxylate
Biological ActivityPF 8380 is a potent autotaxin inhibitor (IC50 = 2.8 nM in isolated enzyme assay; 101 nM in human whole blood). Modulates lysophosphatidic acid (LPA) levels in vivo and in vitro by directly inhibiting autotaxin; reduces LPA levels both in plasma and at site of inflammation. Decreases leptin-induced MMP13 expression, in vitro. Orally available.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Complete Your Research
Autotaxin: its role in biology of melanoma cells and as a pharmacological target.
Enzyme Res., 2011;:194857
A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation.
Gierse et al.
High-fat diet-induced acceleration of osteoarthritis is associated with a distinct and sustained plasma metabolite signature.
Poulami et al.
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