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199113-98-9

中文名称 巴格列酮
英文名称 Balaglitazone
CAS 199113-98-9
分子式 C20H17N3O4S
分子量 395.43
MOL 文件 199113-98-9.mol
199113-98-9 结构式 199113-98-9 结构式

基本信息

中文别名
巴格列酮
英文别名
Nn2344
Drf-2593
Drf 2593
Balaglitazone
Unii-4m1609828o
Balaglitazone [inn]
DRF-2593
NN-2344
DRF2593
NN2344
DRF 2593
NN 2344
(+/-)-5-(p-((3,4-Dihydro-3-methyl-4-oxo-2-quinazolinyl)methoxy)benzyl)-2,4-thiazolidinedione
5-[[4-[(3,4-dihydro-3-methyl-4-oxo-2-quinazolinyl)methoxy]phenyl]methyl]-2,4-Thiazolidinedione
5-[[4-[[3-Methyl-4-oxo-3,4-dihydro-2-quinazolinyl]methoxy]phenyl]methyl]thiazolidine-2,4-dione
所属类别
生物化工:激动剂抑制剂

物理化学性质

密度1.45±0.1 g/cm3(Predicted)
储存条件Inert atmosphere,Store in freezer, under -20°C
溶解度insoluble in H2O; ≥15.45 mg/mL in DMSO; ≥2.18 mg/mL in EtOH with gentle warming and ultrasonic
酸度系数(pKa)6.33±0.50(Predicted)
形态固体
颜色Light yellow to yellow
巴格列酮价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-16086巴格列酮
Balaglitazone
199113-98-95mg1900元
2024/04/30HY-16086巴格列酮
Balaglitazone
199113-98-910mM * 1mLin DMSO2090元
2024/04/30HY-16086巴格列酮
Balaglitazone
199113-98-950mg7812元

常见问题列表

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

PPARγ

351 nM (EC 50 , Human PPARγ)

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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