PF 8380
Chemical Name: 3,5-Dichlorobenzyl-[4-[3-oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]]piperazine-1-carboxylate
Purity: ≥97%
Biological Activity
PF 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Activin-A enhances mTOR signaling to promote aberrant chondrogenesis in fibrodysplasia ossificans progressiva
K Hino, K Horigome, M Nishio, S Komura, S Nagata, C Zhao, Y Jin, K Kawakami, Y Yamada, A Ohta, J Toguchida, M Ikeya
J. Clin. Invest., 2017;0(0):. -
Autotaxin: its role in biology of melanoma cells and as a pharmacological target.
Jankowski
Enzyme Res., 2011;:194857 -
A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation.
Gierse et al.
J.Pharmacol.Exp.Ther., 2010;334:310 -
High-fat diet-induced acceleration of osteoarthritis is associated with a distinct and sustained plasma metabolite signature.
Poulami et al.
Sci.Rep., 2017;7:8205
Product Datasheets
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