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Submit ReviewTesaglitazar
Description: PPARα/γ agonist
Alternative Names: AZ 242
Chemical Name: (S)-2-Ethoxy-3-[4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl]propanoic acid
Purity: ≥98% (HPLC)
Biological Activity for Tesaglitazar
Tesaglitazar is a 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 for Tesaglitazar
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Tesaglitazar
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.85 | 100 | |
| ethanol | 40.85 | 100 |
Preparing Stock Solutions for Tesaglitazar
The following data is based on the product molecular weight 408.47. Batch specific molecular weights may vary from batch to batch due to the degree 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 for Tesaglitazar
References for Tesaglitazar
References are publications that support the biological activity of the product.
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 Ins 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
If you know of a relevant reference for Tesaglitazar, please let us know.
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Keywords: Tesaglitazar, Tesaglitazar supplier, AZ242, peroxisome, proliferator, activated, receptors, ppars, ppara, pparalpha, pparα, pparg, ppargamma, pparγ, agonists, astrazeneca, AZ, 242, Non-selective, PPAR, 3965, Tocris Bioscience
1 Citation for Tesaglitazar
Citations are publications that use Tocris products. Selected citations for Tesaglitazar include:
Fellous et al (2020) Phytocannabinoids promote viability and functional adipogenesis of bone marrow-derived mesenchymal stem cells through different molecular targets Biochemical Pharmacology 175 PMID: 32061773
Do you know of a great paper that uses Tesaglitazar from Tocris? Please let us know.
Reviews for Tesaglitazar
Average Rating: 5 (Based on 1 Review.)
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Tesaglitazar completely abolishes 15d-PGJ2 induced p42/44 activation.
By
Chintan Koyani on 12/10/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: HL-1 cardiomyocytes
HL-1 cardiomyocytes were incubated with Tesaglitazar (10 µM) for 30 min prior to addition of 15 µM 15d-PGJ2 for 30 min. Preincubation of cells with Tesaglitazar completely abolished activation of p42/44 MAPK indicating involvement of PPAR gamma in cellular signalling in response to 15d-PGJ2.
