Balaglitazone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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

Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ.

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.

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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Metabolic Enzyme/Protease

PPAR

PPAR

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199113-98-9

395.43

C20H17N3O4S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (252.89 mM; 超声助溶 )

Cn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc2c1=O

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(-20℃)

With Ice Pack

≥ 2 years