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生物活性 Mifobate (SR-202) 是一种有效且特异性的 PPARγ 拮抗剂，可选择性的抑制噻唑烷二酮 (TZD) 诱导的 PPARγ 转录活性 (IC50=140 μM)。Mifobate 不影响 PPARα，PPARβ 或 FXR 的基础或配体刺激的转录活性。Mifobate 具有抗肥胖和抗糖尿病作用。
靶点

PPARγ

140 μM (IC ₅₀ )
体外研究

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.
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).

体内研究

Mifobate (400 mg/kg; Feed for 20 days) increases insulin sensitivity in ob/ob mice

Animal Model:	Eight-week-old male ob/ob mice
Dosage:	400 mg/kg
Administration:	Feed (food admixture maintained for 20 days)
Result:	Prevented the time-dependent increase in glucose concentrations.

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