SR 1664

一种小分子，可阻断Cdk5对PPARγ的磷酸化（IC50=80nM；Ki=28.7nM），但不表现出PPARγ受体的激动剂活性；在肥胖小鼠中表现出强效的、剂量依赖性的抗糖尿病作用，不会引起体液潴留和体重增加，也不会抑制骨骼形成A small molecule that blocks phosphorylation of PPARγ by Cdk5 (IC50 = 80 nM; Ki = 28.7 nM) without exhibiting agonist activity at the PPARγ receptor; demonstrates potent, dose-dependent anti-diabetic effects in obese mice without inducing fluid retention and weight gain or inhibiting bone formation.