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.
Compound Libraries
Tesaglitazar is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 408.47 |
| Formula | C20H24O7S |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 251565-85-2 |
| PubChem ID | 208901 |
| InChI Key | CXGTZJYQWSUFET-IBGZPJMESA-N |
| Smiles | CS(OC1=CC=C(CCOC2=CC=C(C[C@H](OCC)C(O)=O)C=C2)C=C1)(=O)=O |
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 | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.85 | 100 | |
| ethanol | 40.85 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 408.47. 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 | 2.45 mL | 12.24 mL | 24.48 mL |
| 5 mM | 0.49 mL | 2.45 mL | 4.9 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.45 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: Tesaglitazar, supplier, AZ242, peroxisome, proliferator, activated, receptors, ppars, ppara, pparalpha, pparα, pparg, ppargamma, pparγ, agonists, astrazeneca, AZ, 242, Non-selective, PPAR, Non-selective, PPAR, Tocris Bioscience
