Ambeed 大中华区 CN | ZH

中文 - ZH English - EN

Ambeed.cn

搜索

关键字搜索批量搜索

首页 收藏 购物车0
首页 /
抑制剂/激动剂
药物研究
/
经典阳性药
小分子阳性药 膜转运蛋白
/
钾通道
糖尿病
/ Repaglinide/瑞格列奈

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

货号：A162841 同义名： AG-EE 623ZW

Repaglinide是一种氨基甲基苯甲酸（CMBA）衍生物，可用于2型糖尿病的研究。

Repaglinide/瑞格列奈 化学结构 CAS号：135062-02-1
Repaglinide/瑞格列奈 化学结构
CAS号：135062-02-1
Repaglinide/瑞格列奈 3D分子结构
CAS号：135062-02-1
Repaglinide/瑞格列奈 化学结构 CAS号：135062-02-1
Repaglinide/瑞格列奈 3D分子结构 CAS号：135062-02-1
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} 		{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} 现货 1周 咨询 - +
购物车0 收藏 询单

Repaglinide/瑞格列奈 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:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 Potassium Channel ↓ 其他靶点 纯度
Tolbutamide ✔ 98%
Glimepiride ++++

SUR2B, IC50: 7.3 nM

SUR1, IC50: 5.4 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。

Repaglinide/瑞格列奈 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/瑞格列奈 细胞实验

Cell Line
Concentration Treated Time Description References
Human liver microsome (HLM) 1–500 µM 0, 30, 60 minutes Investigation of RPG metabolism kinetics in HLM, showing saturable and concentration-dependent metabolic profiles fitting Michaelis-Menten kinetics. Vmax was 2380–3240 pmol/min/mg protein, Km was 27.0–69.4 μM, and CLint was 46.6–89.2 μL/min/mg protein. Pharmaceutics. 2021 May 23;13(6):782
Rat liver microsome (RLM) 1–500 µM 0, 30, 60 minutes Investigation of RPG metabolism kinetics in RLM, showing saturable and concentration-dependent metabolic profiles fitting Michaelis-Menten kinetics. Vmax was 1990–4560 pmol/min/mg protein, Km was 16.0–92.2 μM, and CLint was 49.5–124 μL/min/mg protein. Pharmaceutics. 2021 May 23;13(6):782
HEK293 cells (expressing Kir6.2 DN14/SUR1) 51 ± 23 nM 60 minutes To investigate the binding properties of repaglinide to Kir6.2 DN14/SUR1, it was found that repaglinide binds with low affinity (KD=51 ± 23 nM), indicating that the N-terminus of Kir6.2 is crucial for high-affinity binding. Br J Pharmacol. 2005 Feb;144(4):551-7
HEK293 cells 0.42 ± 0.03 nM (high-affinity binding) 60 minutes To investigate the binding properties of repaglinide to SUR1 and Kir6.2/SUR1, it was found that repaglinide binds with low affinity (KD=59 ± 16 nM) to SUR1 alone, but with significantly higher affinity (KD=0.42 ± 0.03 nM) when SUR1 was co-expressed with Kir6.2. Br J Pharmacol. 2005 Feb;144(4):551-7

Repaglinide/瑞格列奈 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats Fasted female Wistar rats Intravenous 0.0003 mg/kg to 0.1 mg/kg (intravenous) Single dose, observed for 180 minutes Repaglinide showed significant hypoglycemic effects in fasted rats with an ED50 value of 3.4 mg kg-1 Br J Pharmacol. 1997 Aug;121(8):1597-604
Adult male albino rats Type 2 diabetes model Transdermal administration 1 mg/kg Single dose, 24 hours duration To evaluate the pharmacokinetic and hypoglycemic activity of REP-SLN-TDDS. Results showed that REP-SLN-TDDS could sustain higher plasma levels and significantly reduce blood glucose levels over 24 hours. Int J Nanomedicine. 2024 Jan 10;19:209-230
C57BL/6J mice High-fat diet/streptozotocin-induced type 2 diabetic mouse model Oral gavage 1 mg/kg/day Daily for 4 weeks To evaluate the effects of Repaglinide alone or in combination with Metformin on blood glucose, liver injury, lipid accumulation, and gut microbiota in type 2 diabetic mice. Results showed that Repaglinide alone or in combination effectively prevented the development of high blood glucose, with combination treatment showing better effects in inhibiting lipid accumulation. BMJ Open Diabetes Res Care. 2024 May 6;12(3):e003837
Mice SOD1G93A transgenic mice Oral 2 µg/mL From week 10 to week 18, drinking water was renewed weekly Repaglinide improved motor strength, reduced motoneuron loss and glial activation in the spinal cord of SOD1G93A mice, and increased ATF6 processing Int J Mol Sci. 2023 Oct 30;24(21):15783
Male Wistar albino rats STZ-induced type 2 diabetes model Oral (via gastric tube) 2 mg/kg Continued for 14 days To evaluate the hypoglycemic effect and pharmacokinetic profile of repaglinide and its liponiosomal hybrids. Results showed that repaglinide-loaded LNHs had higher hypoglycemic efficacy and bioavailability than pure repaglinide. Int J Nanomedicine. 2023 Dec 7;18:7417-7440
Male albino Wistar rats Streptozotocin-induced diabetic rat model Oral 2 mg/kg Single dose, duration of 6 hours Evaluate the hypoglycemic effect of repaglinide. Results showed that Pharmaburst? 500 and F-melt? tablets significantly reduced blood glucose by 5-fold and 3.5-fold at 30 minutes, and sustained reduction by 1.5-fold and 1.3-fold at 6 hours. Drug Deliv. 2023 Dec;30(1):2181747
Sprague-Dawley rats Diabetes model Intravenous and oral intravenous 0.4 mg/kg, oral 0.4 mg/kg Single dose Evaluation of QCT's effect on RPG pharmacokinetics. Results showed significant increases in AUC and Cmax of RPG after concurrent administration with QCT (intravenous AUC increased by 83.4%, oral AUC increased by 87.6%). Pharmaceutics. 2021 May 23;13(6):782

Repaglinide/瑞格列奈 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/瑞格列奈 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/瑞格列奈 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/瑞格列奈 技术信息

CAS号135062-02-1
分子式C27H36N2O4
分子量 452.59
SMILES Code CCOC1=C(C=CC(CC(=O)N[C@@H](CC(C)C)C2=C(C=CC=C2)N2CCCCC2)=C1)C(O)=O
MDL No. MFCD00906179
别名 AG-EE 623ZW
运输蓝冰
InChI Key FAEKWTJYAYMJKF-QHCPKHFHSA-N
Pubchem ID 65981
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

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

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
方案 三

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

AmBeed 相关网站 AmBeed.cn AmBeed.com
AmBeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
    • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    AmBeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质用途提供服务。

    尊敬的 AmBeed 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z