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)

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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
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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Product Datasheets

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References are publications that support the products' biological activity.

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

If you know of a relevant reference for PF 8380, please let us know.

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