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Tesaglitazar

Cat. No. 3965

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Alternative Name: AZ 242

Chemical Name: (S)-2-Ethoxy-3-[4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl]propanoic acid

Biological Activity

Dual-specificity PPARα/γ agonist (IC₅₀ values are 0.35 and 3.8 μM for PPARγ and PPARα respectively). Prevents atherosclerosis progression in E3L.CETP transgenic mice. Also reduces insulin resistance in obese Zucker rats. Orally active.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Technical Data

M.Wt:

408.47

Formula:

C₂₀H₂₄O₇S

Solubility:

Soluble to 100 mM in DMSO and to 100 mM in ethanol

Purity:

>98 %

Storage:

Desiccate at RT

CAS No:

251565-85-2

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Cronet et al (2001) Structure of the PPARβ and -γ ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family. Structure 9 699. PMID: 11587644.

Ljung et al (2002) AZ 242, a novel PPARα/γ agonist with beneficial effects on insulin resistance and carbohydrate and lipid metabolism in ob/ob mice and obese Zucker rats. J.Lipid Res. 43 1855. PMID: 12401884.

Ebdrup et al (2003) Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor α/γ agonist ragaglitazar. J.Med.Chem. 46 1306. PMID: 12672231.

van der Hoorn et al (2009) The dual PPARα/γ agonist tesaglitazar blocks progression of pre-existing atherosclerosis in APOE*3Leiden.CETP transgenic mice. Br.J.Pharmacol. 156 1067. PMID: 19220285.

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