Balaglitazone

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Chemical Structure| 199113-98-9 同义名 : DRF 2593; NN 2344; NNC-61-2344; NNC-61-0645
CAS号 : 199113-98-9
货号 : A117326
分子式 : C20H17N3O4S
纯度 : 99%+
分子量 : 395.432
MDL号 : MFCD09837808
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(265.53 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Balaglitazone is a selective partial agonist of PPARγ with an effective concentration 50 (EC50) of 1.351 μM[1]. Within the concentration range of 5-100 μM, Balaglitazone exhibits uniform cytotoxicity against both K562 and K562/DOX cells. It moderates the toxicity of doxorubicin in these cells, showing IC50 values of 0.117 μM for K562 and 0.53 μM for K562/DOX cells. It is also effective in counteracting multidrug resistance (MDR) in K562/DOX cells. At a concentration of 25 µM, Balaglitazone enhances Rh123 accumulation in K562/DOX cells without affecting MFI in K562 cells. It suppresses P-gp expression in K562/DOX cells through the upregulation of PTEN, a process that can be reversed by PTEN inhibition[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.64mL

2.53mL

1.26mL

25.29mL

5.06mL

2.53mL

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.