AMG131 (INT131) 是一种有效且高度选择性的 PPARγ 部分激动剂，可与 PPARγ 结合，取代罗格列酮，Ki 为~10 nM。 AMG131 可用于研究 2 型糖尿病 (T2DM)。
货号:ajcx34506
CAS:315224-26-1
分子式:C21H12Cl4N2O3S
分子量：514.21
溶解度:DMSO : 250 mg/mL (486.18 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM)[1][2].

AMG131 (INT131) binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM, demonstrating ~20-fold higher affinity than either Rosiglitazone or Pioglitazone, and with greater than 1000-fold selectivity for PPARγ over PPARα, PPARδ, or a set of other nuclear receptors. AMG131 is highly selective for PPARγ, with no binding to PPARα or δ at 10 μM, 1000 fold over the Ki for PPARγ[1].

AMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats following[2]

[1]. Linda S Higgins,et al. The Development of INT131 as a Selective PPARgamma Modulator: Approach to a Safer Insulin Sensitizer. PPAR Res. 2008;2008:936906.
[2]. Alykhan Motani, et al. INT131: a selective modulator of PPAR gamma. J Mol Biol. 2009 Mar 13;386(5):1301-11.