AMG131
规格
| Cas Number | 315224-26-1 |
| 规格或纯度 | ≥99% |
| 纯度 | ≥99% |
| 包装 | 100mg 或 50mg 或 10mg 或 1mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| Action Type | 调节剂 |
| Mechanism Of Action | 过氧化物酶体增殖激活受体伽马调节剂 |
| 溶解性 | DMSO : 250 mg/mL (486.18 mM; Need ultrasonic) |
| 过滤标签 | PPAR,Cell Cycle/DNA Damage,Vitamin D Related/Nuclear Receptor |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | AMG131（INT131）是一种强效、高选择性的 PPARγ 部分激动剂，能与 PPARγ 结合并取代罗格列酮，其 K i 约为 10 nM。AMG131 可用于研究 2 型糖尿病（T2DM）。 |
| 英文描述 |
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. Form:Solid IC50& Target:PPARγ |