Mifobate (SR-202) | PPARγ Antagonist

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.

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