Mifobate 是一种有效且特异性的PPARγ拮抗剂,可选择性抑制噻唑烷二酮 (TZD) 诱导的 PPARγ 转录活性,IC50为140 μM,具有抗肥胖和抗糖尿病作用。
产品描述
Mifobate is a potent and specific antagonist of PPARγ. Mifobate shows antiobesity, antidiabetic and antiatherosclerotic effects[1].
体外活性
SR-202 is a new synthetic PPARgamma antagonist,, which inhibits both TZD-stimulated recruitment of the coactivator steroid receptor coactivator-1 and TZD-induced transcriptional activity of the receptor.?In cell culture, SR-202 efficiently antagonizes hormone- and TZD-induced adipocyte differentiation[1].
体内活性
In vivo, decreasing PPARgamma activity, either by treatment with SR-202 or by invalidation of one allele of the PPARgamma gene, leads to a reduction of both high fat diet-induced adipocyte hypertrophy and insulin resistance.?These effects are accompanied by a smaller size of the adipocytes and a reduction of TNFalpha and leptin secretion.?Treatment with SR-202 also dramatically improves insulin sensitivity in the diabetic ob/ob mice[1].
Cas No.
76541-72-5
分子式
C11H17ClO7P2
分子量
358.65
别名
SR-202;米福贝特
储存和溶解度
H2O:35.87 mg/mL (100.01 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years