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/ Glibenclamide/格列本脲

Glibenclamide/格列本脲 {[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/格列本脲 化学结构 CAS号：10238-21-8
Glibenclamide/格列本脲 化学结构
CAS号：10238-21-8
Glibenclamide/格列本脲 3D分子结构
CAS号：10238-21-8
Glibenclamide/格列本脲 化学结构 CAS号：10238-21-8
Glibenclamide/格列本脲 3D分子结构 CAS号：10238-21-8
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Glibenclamide/格列本脲 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]}
批次查询： 批次纯度:

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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 HCl ✔ 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

 		99%
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 HCl dihydrate ✔ 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

 		99%
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/格列本脲 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/格列本脲 细胞实验

Cell Line
Concentration Treated Time Description References
Mouse peritoneal macrophages 50 µM 6 hours Inhibited LPS-induced NLRP3 inflammasome activation and reduced the secretion of IL-1β and IL-18 Mediators Inflamm. 2022 Feb 11;2022:8457010.

Glibenclamide/格列本脲 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice LPS-induced acute lung injury model Intraperitoneal injection 40 μmol/kg Once daily for 3 days Alleviated LPS-induced lung injury and inhibited the NLRP3 inflammasome signaling pathway Mediators Inflamm. 2022 Feb 11;2022:8457010.

Glibenclamide/格列本脲 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/格列本脲 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/格列本脲 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/格列本脲 技术信息

CAS号10238-21-8
分子式C23H28ClN3O5S
分子量 494.0
SMILES Code O=C(NCCC1=CC=C(S(=O)(NC(NC2CCCCC2)=O)=O)C=C1)C3=CC(Cl)=CC=C3OC
MDL No. MFCD00056625
别名 Glyburide
运输蓝冰
InChI Key ZNNLBTZKUZBEKO-UHFFFAOYSA-N
Pubchem ID 3488
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

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/格列本脲 纯度/质量文件 | Glibenclamide/格列本脲 亚型比较 | Glibenclamide/格列本脲 生物活性 | Glibenclamide/格列本脲 临床数据 | Glibenclamide/格列本脲 参考文献 | Glibenclamide/格列本脲 实验方案 | Glibenclamide/格列本脲 技术信息

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