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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 478.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.09 mL||10.45 mL||20.91 mL|
|5 mM||0.42 mL||2.09 mL||4.18 mL|
|10 mM||0.21 mL||1.05 mL||2.09 mL|
|50 mM||0.04 mL||0.21 mL||0.42 mL|
References are publications that support the biological activity of the product.
Gierse et al (2010) A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation. J.Pharmacol.Exp.Ther. 334 310 PMID: 20392816
Jankowski (2011) Autotaxin: its role in biology of melanoma cells and as a pharmacological target. Enzyme Res. 194857 PMID: 21423677
Poulami et al (2017) High-fat diet-induced acceleration of osteoarthritis is associated with a distinct and sustained plasma metabolite signature. Sci.Rep. 7 8205 PMID: 28811491
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Keywords: PF 8380, PF 8380 supplier, PF8380, pfizer, autotaxin, lysophospholipase, d, inhibitors, lysophosphatidic, acid, LPA, inhibits, potent, Autotaxin, 4078, Tocris Bioscience
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During preliminary studies we investigated whether the ATX inhibitor PF-8380 crosses the BBB and impacts LPA levels in the brain. After oral gavage of 3mg/kg PF-8380 per mouse (PF-8380 was dissolved in hydroxyl methyl cellulose), mice were anesthetized and perfused with PBS at different time points and the whole brains were dissected and immediately snap frozen in liquid nitrogen. Lipids were extracted using the Bligh & Dyer HCl method and the levels of LPA and PF-8380 were quantitated by LC-MS/MS.
Literature in this Area
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