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Balaglitazone

产品编号 TQ0272 CAS 199113-98-9

别名: DRF 2593, 巴格列酮, NN 2344

Balaglitazone is a selective partial agonist for PPARγ (EC50: 1.351 μM for human PPARγ).

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Balaglitazone, CAS 199113-98-9

规格	价格/CNY	货期
2 mg	￥ 932	5日内发货
5 mg	￥ 1,580	5日内发货
10 mg	￥ 2,390	5日内发货
1 mL * 10 mM (in DMSO)	￥ 1,730	5日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Balaglitazone is a selective partial agonist for PPARγ (EC50: 1.351 μM for human PPARγ).
靶点活性	PPARγ (human):1.351 μM
体外活性	Balaglitazone (5-100 μM) has equal cytotoxicity towards K562 and K562/DOX cells. Balaglitazone decreases doxorubicin cytotoxicity in K562 and K562/DOX cells, with IC50s 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 [2].
体内活性	In fully diabetic and insulin-resistant db/db mice, Balaglitazone (3 mg/kg, p.o.) shows antihyperglycaemic activity and is more potent than the full PPARγ agonist rosiglitazone [1]. Balaglitazone (10 mg/kg, p.o.) suppresses overall glucose, decreases insulin levels, and increases body weight in male diet-induced obese rats, and such effects are equal to that of 30 mg/kg pioglitazone [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	DRF 2593, 巴格列酮, NN 2344
分子量	395.43
分子式	C20H17N3O4S
CAS No.	199113-98-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 480 mg/mL (1213.87 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5289 mL	12.6445 mL	25.2889 mL	63.2223 mL
	5 mM	0.5058 mL	2.5289 mL	5.0578 mL	12.6445 mL
	10 mM	0.2529 mL	1.2644 mL	2.5289 mL	6.3222 mL
	20 mM	0.1264 mL	0.6322 mL	1.2644 mL	3.1611 mL
	50 mM	0.0506 mL	0.2529 mL	0.5058 mL	1.2644 mL
	100 mM	0.0253 mL	0.1264 mL	0.2529 mL	0.6322 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

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容积 (起始)

浓度 (终)

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参考文献

1. Larsen PJ, et al. Dissociation of antihyperglycaemic and adverse effects of partial perioxisome proliferator-activated receptor (PPAR-gamma) agonist balaglitazone. Eur J Pharmacol. 2008 Oct 31;596(1-3):173-9. 2. Yousefi B, et al. Balaglitazone reverses P-glycoprotein-mediated multidrug resistance via upregulation of PTEN in a PPARγ-dependent manner in leukemia cells. Tumour Biol. 2017 Oct;39(10):1010428317716501. 3. Henriksen K, et al. A comparison of glycemic control, water retention, and musculoskeletal effects of balaglitazone and pioglitazone in diet-induced obese rats. Eur J Pharmacol. 2009 Aug 15;616(1-3):340-5.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：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

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Balaglitazone 199113-98-9 DNA Damage/DNA Repair Metabolism PPAR DRF 2593 巴格列酮 DRF2593 NN2344 NN 2344 DRF-2593 NN-2344 Inhibitor inhibitor inhibit

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Balaglitazone

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

剂量换算

体内实验配液计算器

技术支持

Keywords