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Repaglinide

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Chemical Structure| 135062-02-1 同义名 : AG-EE 623ZW
CAS号 : 135062-02-1
货号 : A162841
分子式 : C27H36N2O4
纯度 : 98%
分子量 : 452.586
MDL号 : MFCD00906179
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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

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].
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 <<
实验方案
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
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