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Balaglitazone

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产品编号 TQ0272Cas号 199113-98-9
别名 巴格列酮, NN-2344, NN2344, NN 2344, DRF-2593, DRF2593, DRF 2593

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

Balaglitazone

Rating icon 很棒
纯度: 99.74%
产品编号 TQ0272 别名 巴格列酮, NN-2344, NN2344, NN 2344, DRF-2593, DRF2593, DRF 2593Cas号 199113-98-9

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。

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产品介绍

生物活性
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
化学信息
分子量395.43
分子式C20H17N3O4S
CAS No.199113-98-9
SmilesCn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc2c1=O
密度1.45 g/cm3 (Predicted)
储存&溶解度
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
1mg5mg10mg50mg
1 mM2.5289 mL12.6445 mL25.2889 mL126.4446 mL
5 mM0.5058 mL2.5289 mL5.0578 mL25.2889 mL
10 mM0.2529 mL1.2644 mL2.5289 mL12.6445 mL
20 mM0.1264 mL0.6322 mL1.2644 mL6.3222 mL
50 mM0.0506 mL0.2529 mL0.5058 mL2.5289 mL
100 mM0.0253 mL0.1264 mL0.2529 mL1.2644 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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