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Glibenclamide

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Chemical Structure| 10238-21-8 同义名 : Glyburide
CAS号 : 10238-21-8
货号 : A212350
分子式 : C23H28ClN3O5S
纯度 : 98%
分子量 : 494.003
MDL号 : MFCD00056625
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(212.55 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
靶点

  • Potassium Channel
描述 Glibenclamide (Gli) is a selective inhibitor of ATP-sensitive K+ channel. Gli inhibited cell proliferation assessed by a clonogenic method in a dose dependent manner, with an increment in the population doubling time. When cell cycle analysis was performed by flow cytometry, Gli induced a significant cell-cycle arrest in G0/G1 phase, together with an up-regulation of p27 levels and a diminution in cyclin E expression, both evaluated by immunoblot[3]. The GLUT1 expression was found to be affected by the glucose and insulin levels and can be modulated by glibenclamide in severely and mildly diabetic rats. Glibenclamide can prevent the liver damage caused by severe hyperglycemia[4]. Glibenclamide caused more hypoglycemia than other secretagogues and other sulfonylureas. Glibenclamide was not associated with an increased risk of cardiovascular events, death, or weight gain[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO cells Function assay Inhibition of human SUR1/Kir6.2 expressed in CHO cells, IC50=0.0043 μM 11356099
HEK293 cells Function assay Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate, IC50=1.4 μM 22587986
INS-1E cells Function assay 1 h Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose, EC50=0.003 μM 24484900
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00347100 Diabetes Mellitus, Type 2 Phase 4 Completed - China ... 展开 >> Sanofi-Aventis Beijing, China 收起 <<
NCT01706211 Diabetes Mellitus Non Insulin ... 展开 >>Dependent Oral Agent Therapy 收起 << Phase 3 Completed - Taiwan ... 展开 >> National Taiwan University Hospital Taipei, Taiwan, 10002 收起 <<
NCT00608179 Type 2 Diabetes Not Applicable Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.12mL

2.02mL

1.01mL

20.24mL

4.05mL

2.02mL
参考文献

[1]Nieland TJ, Chroni A, et al. Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide. J Lipid Res. 2004 Jul;45(7):1256-65.

[2]Winquist RJ, Heaney LA, et al. Glyburide blocks the relaxation response to BRL 34915 (cromakalim), minoxidil sulfate and diazoxide in vascular smooth muscle. J Pharmacol Exp Ther. 1989 Jan;248(1):149-56.

[3]Núñez M, Medina V, Cricco G, et al. Glibenclamide inhibits cell growth by inducing G0/G1 arrest in the human breast cancer cell line MDA-MB-231. BMC Pharmacol Toxicol. 2013;14:6. Published 2013 Jan 11

[4]Sokolovska J, Isajevs S, Sugoka O, et al. Comparison of the effects of glibenclamide on metabolic parameters, GLUT1 expression, and liver injury in rats with severe and mild streptozotocin-induced diabetes mellitus. Medicina (Kaunas). 2012;48(10):532-543

[5]Gangji AS, Cukierman T, Gerstein HC, Goldsmith CH, Clase CM. A systematic review and meta-analysis of hypoglycemia and cardiovascular events: a comparison of glyburide with other secretagogues and with insulin. Diabetes Care. 2007;30(2):389-394