PF 8380

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Cat.No. 4078 - PF 8380 | C22H21Cl2N3O5 | CAS No. 1144035-53-9
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)
Datasheet
Citations
Reviews (1)
Literature

Biological Activity

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

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 47.83 100

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

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References

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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Reviews for PF 8380

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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.

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