Cas No.: | 76541-72-5 |
Synonyms: | SR-202;SR 202;SR202 |
SMILES: | O=P(OC(P(=O)(OC)OC)C1C=CC(Cl)=CC=1)(OC)OC |
Formula: | C11H17ClO7P2 |
M.Wt: | 358.65 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [1]. Rieusset J, et al. A new selective peroxisome proliferator-activated receptor gamma antagonist with antiobesityand antidiabetic activity. Mol Endocrinol. 2002 Nov;16(11):2628-44. |
Description: | Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects[1]. |
Target: | PPARγ:140 μM (IC50) |
In Vivo: | Mifobate (400 mg/kg; Feed for 20 days) increases insulin sensitivity in ob/ob mice[1] Animal Model: Eight-week-old male ob/ob mice[1] Dosage: 400 mg/kg Administration: Feed (food admixture maintained for 20 days) Result: Prevented the time-dependent increase in glucose concentrations. |
In Vitro: | Mifobate (100-400 μM; pretreated with 24 hours) significantly inhibits BRL 49653- and hormone-induced adipocyte differentiation of 3T3-L1 cells in a dose-dependent manner after 6 days[1]. Mifobate is able to both interact specifically with PPARγ and inhibit its agonist-dependent interaction with the coactivator steroid receptor coactivator-1 (SRC-1). Mifobate (SR-202) inhibits TZD-stimulated recruitment of the coactivator steroid receptor coactivator-1. Mifobate blocks adipocyte differentiation induced either by thiazolidinediones or by the combination of dexamethasone, insulin, and 3-isobutyl-1-methylxanthine (IBMX)[1]. |
References: | [1]. Rieusset J, et al. A new selective peroxisome proliferator-activated receptor gamma antagonist with antiobesityand antidiabetic activity. Mol Endocrinol. 2002 Nov;16(11):2628-44. |