Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ.
IC50&Target
PPARγ
351 nM (EC50, Human PPARγ)
体外研究
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.
体内研究
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.
分子式
C20H17N3O4S
分子量
395.43
CAS号
199113-98-9
中文名称
巴格列酮
运输条件
Room temperature in continental US; may vary elsewhere.