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/ Repaglinide

瑞格列奈 /Repaglinide {[allProObj[0].p_purity_real_show]}

货号：A162841 同义名： AG-EE 623ZW

Repaglinide is a carbamoylmethyl benzoic acid (CMBA) derivative, which recently has become available for the treatment of type II diabetes.

Repaglinide 化学结构 CAS号：135062-02-1
Repaglinide 化学结构
CAS号：135062-02-1
Repaglinide 3D分子结构
CAS号：135062-02-1
Repaglinide 化学结构 CAS号：135062-02-1
Repaglinide 3D分子结构 CAS号：135062-02-1
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Repaglinide 纯度/质量文件 产品仅供科研

货号：A162841 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 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。

Repaglinide 生物活性

靶点

  • Potassium Channel
描述 Repaglinide is an insulin secretagogue for the treatment of type-2 diabetes mellitus. Repaglinide reduces postprandial glucose levels by enhancing the early phase of insulin secretion and increasing the total amount of insulin secreted. Furthermore, Repaglinide is inactivated in the liver and more than 90% excreted via the bile. Repaglinide (1 mg/kg p.o.) is effective as an insulin-releasing agent in a rat model (low-dose streptozotocin) of type 2 diabetes[3]. Repaglinide lowers fasting and postprandial blood glucose levels in animals, healthy volunteers and patients with type 2 diabetes mellitus. Repaglinide is rapidly absorbed and eliminated, which may allow a relatively fast onset and offset of action. Excretion occurs almost entirely by non-renal mechanisms. In comparative clinical trials in patients with type 2 diabetes mellitus, repaglinide 0.5 to 4 mg twice or 3 times daily before meals provided similar glycaemic control to glibenclamide (glyburide) 2.5 to 15 mg/day[4]. Moreover, repaglinide significantly reduced Bcl-2, Beclin-1 and PD-L1 expression in glioma tissues, indicating that repaglinide may exert its anti-cancer effects via apoptotic, autophagic and immune checkpoint signaling[5].

Repaglinide 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
NCT03492580 - Completed - United States, New Jersey ... 展开 >> Janssen Investigative Site Titusville, New Jersey, United States, 08560 收起 <<
NCT01974544 Type 2 Diabetes Not Applicable Unknown December 2016 Chile ... 展开 >> Pontificia Universidad Católica de Chile Recruiting Santiago, Región Metropolitana, Chile, 8330033 Contact: Castillo Alejandra, Nurse    56223543527    macastia@uc.cl    Contact: Vega Andrea, Nurse    56223543879    abvega@uc.cl    Principal Investigator: Boza Camilo, MD surgeon          Sub-Investigator: Valderas Juan Patricio, MD          Sub-Investigator: Arrese Marco, MD Internist          Sub-Investigator: Muñoz Rodrigo, MD 收起 <<
NCT02456428 - Completed - Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 <<

Repaglinide 参考文献

[1]Hansen AM, Hansen JB, et al. Kir6.2-dependent high-affinity repaglinide binding to beta-cell K(ATP) channels. Br J Pharmacol. 2005 Feb;144(4):551-7.

[2]Okada M, Takezawa D, et al. Neuronal calcium sensor proteins are direct targets of the insulinotropic agent repaglinide. Biochem J. 2003 Oct 1;375(Pt 1):87-97.

[3]Wang LC, Fang FS, Gong YP, Yang G, Li CL. Characteristics of repaglinide and its mechanism of action on insulin secretion in patients with newly diagnosed type-2 diabetes mellitus. Medicine (Baltimore). 2018;97(38):e12476

[4]Balfour JA, Faulds D. Repaglinide [published correction appears in Drugs Aging 1999 Jul;15(1):28]. Drugs Aging. 1998;13(2):173-180

[5]Xiao ZX, Chen RQ, Hu DX, Xie XQ, Yu SB, Chen XQ. Identification of repaglinide as a therapeutic drug for glioblastoma multiforme. Biochem Biophys Res Commun. 2017;488(1):33-39

Repaglinide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.05mL

2.21mL

1.10mL

22.10mL

4.42mL

2.21mL

Repaglinide 技术信息

CAS号135062-02-1
分子式C27H36N2O4
分子量 452.586
别名 AG-EE 623ZW
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 50 mg/mL(110.48 mM)，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

PO 5% DMSO+2% Tween80+30% PEG300+water 0.3 mg/mL clear

Tags: Repaglinide | 135062-02-1 | AG-EE 623ZW | Membrane Transporter/Ion Channel | Potassium Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Repaglinide 纯度/质量文件 | Repaglinide 亚型比较 | Repaglinide 生物活性 | Repaglinide 临床数据 | Repaglinide 参考文献 | Repaglinide 实验方案 | Repaglinide 技术信息

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