中文名 | Balaglitazone |
英文名 | Balaglitazone |
别名 | 巴格列酮 5-(4-((3-甲基-4-氧代-3,4-二氢喹唑啉-2-基)甲氧基)苄基)噻唑烷-2,4-二酮 |
英文别名 | Nn2344 Drf-2593 Drf 2593 Balaglitazone Unii-4m1609828o Balaglitazone [inn] 2,4-Thiazolidinedione,5-[[4-[(3,4-dihydro-3-methyl-4-oxo-2-quinazolinyl) methoxy]phenyl]methyl]- |
CAS | 199113-98-9 |
化学式 | C20H17N3O4S |
分子量 | 395.43 |
密度 | 1.45±0.1 g/cm3(Predicted) |
酸度系数 | 6.33±0.50(Predicted) |
存储条件 | Inert atmosphere,Store in freezer, under -20°C |
体外研究 | Balaglitazone is a selective partial PPARγ agonist with an EC 50 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 IC 50 s 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. |
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