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Balaglitazone 是一种选择性的过氧化物酶体增殖物激活受体(PPARγ)部分激动剂,对人 PPARγ 的 EC50 值为 1.351 μM。Balaglitazone 可作为胰岛素治疗的补充剂,可调节血糖,可用于研究心力衰竭和心肌梗塞。
Balaglitazone 是一种选择性的过氧化物酶体增殖物激活受体(PPARγ)部分激动剂,对人 PPARγ 的 EC50 值为 1.351 μM。Balaglitazone 可作为胰岛素治疗的补充剂,可调节血糖,可用于研究心力衰竭和心肌梗塞。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 638 | 现货 |
产品描述 | Balaglitazone is a selective peroxisome proliferator-activated receptor (PPARγ) partial agonist with an EC50 value of 1.351 μM for human PPARγ.Balaglitazone can be used as a supplement to insulin therapy, regulates blood glucose, and can be used in studies of heart failure and myocardial infarction. |
靶点活性 | PPARγ (human):351 μM (EC50) |
体外活性 | Balaglitazone在 K562 和 K562/DOX 细胞中表现出相等的细胞毒性,其 IC50 分别为 0.117 μM和 0.53 μM,并能降低 Doxorubicin 对这些细胞的细胞毒性[2]。 |
体内活性 | Balaglitazone 在雄性饮食诱导性肥胖大鼠中(口服10 mg/kg)抑制总体血糖,降低胰岛素水平,并增加体重,其效果与口服30 mg/kg吡格列酮相当[3]。 |
细胞实验 | MTT assay is used for cell viability analyses. Briefly, K562 and K562/DOX cells are seeded in a 96-well plate in RPMI-1640 medium supplemented with 10% FBS at the density of 2 × 104 cells/well. After 24 h incubation, various concentrations of doxorubicin (DOX) with or without balaglitazone are diluted in RPMI-1640 medium (without FBS) and added into each well. Experiments for each group are performed in triplicates and with a blank control. After 48 h of treatment, the medium is removed and 200 μL of RPMI-1640 medium supplemented with 10% FBS and 10% MTT (5 mg/mL) is added. After incubation for another 4 h, the reduced intracellular formazan product is dissolved by replacing 100 μL of RPMI-1640 medium with the same volume of dimethyl sulfoxide (DMSO). Absorbance values are measured at 570 nm with a microplate reader. The half-maximal inhibitory concentration (IC50) of each experiment is calculated. The resistance fold (RF) is calculated by dividing the IC50 value of treatment in resistant cells by the IC50 value of treatment in corresponding parental cells [2]. |
动物实验 | Antihyperglycaemic effects of balaglitazone and rosiglitazone are assessed in adult male diabetic db/db mice. At 14 weeks of age, animals are randomized according to fasting blood glucose into 11 groups (n = 6). Mice are dosed orally once daily for 9 days with vehicle (0.2% carboxymethyl cellulose (CMC) + 0.4% Tween-80 in saline) or increasing doses of either balaglitazone (0.1; 0.3; 1.0; 3.0; 10.0 mg/kg/day) or rosiglitazone (0.2; 0.6; 2.0; 6.0 mg/kg/day). After 7 days of treatment, plasma samples obtained in the morning (between 8:00 and 10:00 AM) are analyzed for glucose and insulin. After 9 days of treatment, animals are exposed to an oral glucose tolerance test (OGTT; 3.0 g/kg). The resulting area under the curve is calculated for each of the doses [1]. |
别名 | 巴格列酮, NN-2344, NN2344, NN 2344, DRF-2593, DRF2593, DRF 2593 |
分子量 | 395.43 |
分子式 | C20H17N3O4S |
CAS No. | 199113-98-9 |
Smiles | Cn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc2c1=O |
密度 | 1.45 g/cm3 (Predicted) |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 80 mg/mL (202.31 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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