Balaglitazone巴格列酮,199113-98-9

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Balaglitazone

CAS No. : 199113-98-9

MCE 国际站：Balaglitazone

产品活性：Balaglitazone 是一种选择性的 PPARγ 部分激动剂，对人 PPARγ 的 EC₅₀ 值为 1.351 μM。

研究领域：Cell Cycle/DNA Damage  |  Vitamin D Related/Nuclear Receptor

作用靶点：PPAR

In Vitro: Balaglitazone is a selective partial PPARγ agonist with an EC₅₀ of 1.351 μM. Balaglitazone (5-100 μM) has equal cytotoxicity towards K562 and K562/DOX cells. Balaglitazone decreases doxorubicin cytotoxicity in K562 and K562/DOX cells, with IC₅₀s of 0.117 μM and 0.53 μM, respectively. Balaglitazone reverses multidrug resistance (MDR) in K562/DOX cells. Balaglitazone (25 µM) increases Rh123 accumulation in K562/DOX cells, but does not increases MFI in K562 cells. Balaglitazone downregulates P-gp expression in K562/DOX cells, and such effects are via upregulation of PTEN in K562/DOX cells, and be abolished by PTEN inhibition.

In Vivo: Balaglitazone (3 mg/kg, p.o.) shows antihyperglycaemic activity in fully diabetic and insulin resistant db/db mice, and is more potent than the full PPARγ agonist rosiglitazone. Balaglitazone (10 mg/kg, p.o.) suppresses overall glucose, decreases insulin levels, and increases bodyweight in male diet-induced obese rats, and such effects are equal to that of 30 mg/kg pioglitazone.

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