Biological Activity
Selective PPARγ antagonist; antidiabetic and antiobesity agent. Attenuates troglitazone-induced PPARγ transcriptional activity (IC50 = 140 μM) without affecting ligand-stimulated PPARα, PPARβ or FXR transcriptional activity. Inhibits PPARγ-dependent adipocyte differentiation and growth in vitro and in vivo. Improves insulin sensitivity in diabetic ob/ob mice and increases HDL levels in rats in vivo.
Technical Data
| M. Wt | 358.65 |
| Formula | C11H17ClO7P2 |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 76541-72-5 |
| PubChem ID | 60910 |
| InChI Key | VQHUQHAPWMNBLP-UHFFFAOYSA-N |
| Smiles | COP(=O)(OC)OC(C1=CC=C(Cl)C=C1)P(=O)(OC)OC |
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 | |||
| water | 35.87 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 358.65. 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 | 2.79 mL | 13.94 mL | 27.88 mL |
| 5 mM | 0.56 mL | 2.79 mL | 5.58 mL |
| 10 mM | 0.28 mL | 1.39 mL | 2.79 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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References
References are publications that support the products' biological activity.
Nguyen et al (1987) gem-Diphosphonate and gem-phosphonate-phosphate compounds with specific high density lipoprotein inducing activity. J.Med.Chem. 30 1426 PMID: 3612689
Rieusset et al (2002) A new selective peroxisome proliferator-activated receptor γ antagonist with antiobesity and antidiabetic activity. Mol.Endocrinol. 16 2628 PMID: 12403851
Doggrell (2003) Do peroxisome proliferation receptor-γ antagonists have clinical potential as combined antiobesity and antidiabetic drugs? Expert.Opin.Invest.Drugs 12 713 PMID:
Keywords: SR 202, supplier, Selective, PPARγ, PPARgamma, antagonists, antidiabetic, antiobesity, agent, Peroxisome, Proliferator-activating, Receptors, SR202, Mifobate, PPARgamma, Receptors, PPARgamma, Receptors, Tocris Bioscience
