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Submit ReviewPF 8380
Description: Potent autotaxin inhibitor
Chemical Name: 3,5-Dichlorobenzyl-[4-[3-oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]]piperazine-1-carboxylate
Purity: ≥97% (HPLC)
Biological Activity for PF 8380
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 for PF 8380
| M. Wt | 478.33 |
| Formula | C22H21Cl2N3O5 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 1144035-53-9 |
| PubChem ID | 25265312 |
| InChI Key | JMSUDQYHPSNBSN-UHFFFAOYSA-N |
| Smiles | O=C(C2=CC(OC(N4)=O)=C4C=C2)CCN1CCN(C(OCC3=CC(Cl)=CC(Cl)=C3)=O)CC1 |
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.
Product Datasheets for PF 8380
References for PF 8380
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
Citations for PF 8380
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Currently there are no citations for PF 8380.
Reviews for PF 8380
Average Rating: 5 (Based on 2 Reviews.)
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The effect of ATX inhibition on LPS induced pro-inflammatory phenotype in microglia..
By
lisha joshi on 06/10/2019
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: BV2 microglia cells
PF8380 was used to inhibit autotaxin in BV2 microglia cells in order to study the effect of ATX-LPA axis on microglia proinflammatory phenotype. Cells were treated with LPS (20ng/mi) in the absence or presence of the inhibitor (10µM) for 24 hours and then collected for RNA isolation and subsequent analysis of iNOS and TNFa expression with qPCR.
PF 8380 decreases the levels of lysophosphatidic acid in mouse brain.
By
Joanna Plastira on 10/10/2018
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: Brain
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.
