Chiglitazar sodium  (Synonyms: Carfloglitazar sodium)

Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC₅₀s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.

Chiglitazar 与 Rosiglitazone 和 Pioglitazone 对 PPARγ 以及 WY14643 对 PPARα 进行了比较剂量反应研究。Chiglitazar 显示两种亚型的显著激活。Chiglitazar 的 PPARγ 激活活性弱于 Rosiglitazone，但强于 Pioglitazone。在 PPARα 激活方面，Chiglitazar 显示出比 Rosiglitazone、Pioglitazone 或选择性 PPARα 激动剂 WY14643 更有效的活性^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

注射胰岛素后，与用载体处理的对照组相比，用 Chiglitazar 或 Rosiglitazone 处理的 MSG 大鼠的血浆葡萄糖水平在所有时间点均显著降低。用 Chiglitazar 和 Rosiglitazone 处理的动物的空腹 PI 水平低于对照。用 Chiglitazar 和 Rosiglitazone 处理的 MSG 肥胖大鼠的 ISI 显著高于对照组。此外，Chiglitazar 改善了 HOMA 指数。对于 IPGTT，在葡萄糖负荷后 30 分钟，5 和 10 mg / kg Chiglitazar 和 Rosiglitazone 处理组的葡萄糖值显著低于载体处理组。处理组 IPGTT 期间葡萄糖反应积分显著低于对照组^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

594.61

C₃₆H₂₈FN₂NaO₄

2390374-10-2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Li PP, et al. The PPARalpha/gamma dual agonist chiglitazar improves insulin resistance and dyslipidemia in MSG obese rats. Br J Pharmacol. 2006 Jul;148(5):610-8.  [Content Brief]

  [2]. He BK, et al. In Vitro and In Vivo Characterizations of Chiglitazar, a Newly Identified PPAR Pan-Agonist. PPAR Res. 2012;2012:546548.  [Content Brief]