计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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Moligand™ 级 ,适用于对基线干扰要求严格的色谱和分析工作流程。
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a K i of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM)
In Vitro
AMG131 (INT131) binds to PPARγ and displaces Rosiglitazone with a K i 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 K i for PPARγ. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats followingMCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Zucker fatty (fa/fa) rats ages 7-8 weeksDosage: 80 mg/kg Administration: Administered once daily by oral gavage for 14 days Result: Exhibited maximal efficacy comparable to that of Rosiglitazone with respect to plasma glucose clearance in an oral glucose tolerance test. Reduced baseline insulin levels, similar to Rosiglitazone, could improve insulin sensitivity in treated animals.
IC50& Target:PPARγ
| ALogP | 6.8 |
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
| 分析证书 | A656660 |