巴格列酮
中文名称 | 巴格列酮 |
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中文同义词 | 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 |
英文名称 | Balaglitazone |
英文同义词 | Balaglitazone;2,4-Thiazolidinedione,5-[[4-[(3,4-dihydro-3-methyl-4-oxo-2-quinazolinyl) methoxy]phenyl]methyl]-;(+/-)-5-(p-((3,4-Dihydro-3-methyl-4-oxo-2-quinazolinyl)methoxy)benzyl)-2,4-thiazolidinedione;Balaglitazone [inn];Drf 2593;Drf-2593;Nn2344;Unii-4m1609828o |
CAS号 | 199113-98-9 |
分子式 | C20H17N3O4S |
分子量 | 395.43 |
EINECS号 | |
相关类别 | 原料药;细胞周期;APIs |
Mol文件 | 199113-98-9.mol |
结构式 |
巴格列酮 性质
密度 | 1.45±0.1 g/cm3(Predicted) |
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储存条件 | Inert atmosphere,Store in freezer, under -20°C |
溶解度 | 不溶于水; DMSO 中≥15.45 mg/mL;温和加热和超声波下,乙醇中≥2.18 mg/mL |
形态 | 固体 |
酸度系数(pKa) | 6.33±0.50(Predicted) |
PPARγ 351 nM (EC 50 , Human PPARγ) |
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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/25 | HY-16086 | 巴格列酮 Balaglitazone | 199113-98-9 | 5mg | 1900元 |
2024/01/25 | HY-16086 | 巴格列酮 Balaglitazone | 199113-98-9 | 10mM * 1mLin DMSO | 2090元 |