SR 1664
货号：
11086-1mg 基本售价：
504.0 元 规格：
1 mg
产品信息
概述| 货号 | 11086-1mg |
| 描述 | Apart from direct peroxisome proliferator-activated receptor γ (PPARγ) agonism, several PPARγ ligands have recently been shown to exert anti-diabetic effects through a second, distinct biochemical function: blocking the obesity-linked phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) at serine 273.1 This effect requires binding to the PPARγ ligand binding domain, which causes a conformational change that interferes with the ability of Cdk5 to phosphorylate serine 273. SR 1664 is a small molecule that blocks phosphorylation of peroxisome proliferator-activated receptor γ (PPARγ) by cyclin-dependent kinase 5 with an IC50 value of 80 nM (Ki = 28.7 nM) without exhibiting agonist activity at the PPARγ receptor.2 It demonstrates potent, dose-dependent anti-diabetic effects in obese mice without inducing fluid retention and weight gain or inhibiting bone formation.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Norris, A.W. and Sigmund, C.D. A second chance for a PPARγ targeted therapy?: A commentary on "antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation". Circulation Research 110(1), 8-11 (2012).
2.Choi, J.H.,Banks, A.S.,Kamenecka, T.M., et al. Anti-diabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation. Nature 477(7365), 477-481 (2012).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 547.6 |
| 分子式 | C33H29N3O5 |
| CAS号 | 1338259-05-4 |
| 稳定性 | ≥ 2 years |
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