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/ Glibenclamide

格列本脲 /Glibenclamide {[allProObj[0].p_purity_real_show]}

货号：A212350 同义名： Glyburide

Glibenclamide (Glyburide)是一种口服活性ATP敏感的K+通道（KATP）抑制剂，用于糖尿病和肥胖研究。它抑制P-糖蛋白，直接结合并阻断KATP的SUR1亚基，抑制囊性纤维化跨膜传导调节蛋白（CFTR），通过改变膜离子通透性干扰线粒体生物能量学，并能诱导自噬。

Glibenclamide 化学结构 CAS号：10238-21-8
Glibenclamide 化学结构
CAS号：10238-21-8
Glibenclamide 3D分子结构
CAS号：10238-21-8
Glibenclamide 化学结构 CAS号：10238-21-8
Glibenclamide 3D分子结构 CAS号：10238-21-8
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Glibenclamide 纯度/质量文件 产品仅供科研

货号：A212350 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 Potassium Channel ↓ 其他靶点 纯度
Tolbutamide ✔ 98%
Glimepiride ++++

SUR1, IC50: 5.4 nM

SUR2B, IC50: 7.3 nM

 		97%
Dronedarone Hydrochloride ✔ 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

 		98%
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

 		98%
Glibenclamide ✔ 98%
Amiodarone HCl ✔ 97%
Gliclazide ++

Potassium channel, IC50: 184 nM

 		98%
Repaglinide ✔ 98%
Dofetilide ✔ 98%
Nateglinide ✔ 99%
Quinine hydrochloride dihydrate ✔ 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

 		97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Glibenclamide 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].

Glibenclamide 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

Glibenclamide 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 - -

Glibenclamide 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

Glibenclamide 实验方案

计算器
存储液制备 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

Glibenclamide 技术信息

CAS号10238-21-8
分子式C23H28ClN3O5S
分子量 494.003
别名 Glyburide
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
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

Tags: Glibenclamide | 10238-21-8 | Glyburide | KATP Inhibitor | Membrane Transporter/Ion Channel | Metabolic Enzyme/Protease | Autophagy | Potassium Channel | Mitochondrial Metabolism | Autophagy | CFTR | P-glycoprotein | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Glibenclamide 纯度/质量文件 | Glibenclamide 亚型比较 | Glibenclamide 生物活性 | Glibenclamide 细胞研究 | Glibenclamide 临床数据 | Glibenclamide 参考文献 | Glibenclamide 实验方案 | Glibenclamide 技术信息

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