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AMG131
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AMG131图片
CAS NO:315224-26-1
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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)。
Cas No.315224-26-1
别名2,4-二氯-N-[3,5-二氯-4-(喹啉-3-基氧基)苯基]苯磺酰胺,INT131
分子式C21H12Cl4N2O3S
分子量514.21
溶解度DMSO : 250 mg/mL (486.18 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.