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Chiglitazar

CAS No. : 743438-45-1

MCE 站：Chiglitazar

产品活性：Chiglitazar 是泛过氧化物酶体增殖物激活受体 (PPARα/γ) 的双抑制剂，其对PPARα，PPARγ 和 PPARδ 的 EC₅₀ 值分别为 1.2，0.08 和 1.7 μM。

研究领域：Cell Cycle/DNA Damage

作用靶点：PPAR

In Vitro: Comparative dose-response study of Chiglitazar is performed with rosiglitazone and pioglitazone for PPARγ, and WY14643 for PPARα. Chiglitazar shows significant activation of both the isoforms. Chiglitazar shows weaker PPARγ activating activity than rosiglitazone, but stronger than pioglitazone. In terms of PPARα activation, Chiglitazar shows more potent activity than rosiglitazone, pioglitazone, or WY14643 which is a selective PPARα agonist.

In Vivo: After insulin injection, plasma glucose levels in the MSG rats treated with Chiglitazar or rosiglitazone are significantly reduced compared with the control group treated with vehicle at all time points. Fasting PI levels are lower in animals treated with Chiglitazar and rosiglitazone than control. The ISIs of MSG obese rats treated with chiglitazar and rosiglitazone are significantly higher than control. Furthermore, Chiglitazar ameliorates the HOMA indices. For IPGTT, at the 30?min after glucose loading, the glucose values in the 5 and 10?mg?/kg Chiglitazar and rosiglitazone-treatment groups are significantly lower than those in the vehicle treatment group. The integrated for the glucose response during the IPGTT in the treatment groups are significantly less than those in the control groups.

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