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抑制剂 > 蛋白酵素 > Imeglimin hydrochloride
产品名称:
Imeglimin hydrochloride
型号:
CS-01Y64775
生产地址
进口、国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

10 mM * 1 mL in DMSO 2mg 5mg 10mg 50mg

CAS

775351-61-6

别名

N/A

化学名

(R)-6-imino-N,N,4-trimethyl-1,4,5,6-tetrahydro-1,3,5-triazin-2-amine hydrochloride

分子式

C6H14ClN5

分子量

191.66

溶解度

29.9mg/mL in DMSO

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                             

AMP-activated protein kinase (AMPK) acts as an integrator of regulatory signals to monitor systemic and cellular energy status. Imeglimin targets on three main organs involved in glucose homeostasis: liver, muscle and the pancreas and thus has a distinct mode of action in comparison to existing Type 2 diabetes treatments.

In vitro: In liver mitochondria, imeglimin redirects substrate flows in favor of complex II. Moreover, imeglimin inhibits complex I and restores complex III activities, advicing an increase of fatty acid oxidation, further supported by an increase in hepatic 3-hydroxyacetyl-CoA dehydrogenase activity and acylcarnitine profile. Imeglimin was also found to reduce the production of reactive oxygen species and increases the DNA of mitochondrial [1].

In vivo: A previous study used a model of 16-week high-fat, high-sucrose diet (HFHSD) mice to characterize imeglimin's antidiabetic effects. Six-week imeglimin treatment could decrease glycemia, restore normal glucose tolerance, and improve insulin sensitivity, body weights and food intake significantly. This was associated with an increase of insulin-stimulated protein kinase B phosphorylation in the liver and muscle. In conclusion, imeglimin could normalize glucose tolerance and insulin sensitivity via preserving mitochondrial function from oxidative stress and favoring lipid oxidation in liver of HFHSD mice [1].

Clinical trial: Imeglimin is an experimental drug being developed as an oral anti-diabetic. Imeglimin is in development (completed phase IIb clinical trials) for use both as monotherapy and in combination with other type-2 diabetes treatments. Various research protocols are being known through various scientists. Early studies showed that imeglimin is as effective as metformin in regulating glycaemic control.

Reference:

[1] Vial G, Chauvin MA, Bendridi N, Durand A, Meugnier E, Madec AM, Bernoud-Hubac N, Pais de Barros JP, Fontaine é, Acquaviva C, Hallakou-Bozec S, Bolze S, Vidal H, Rieusset J.Imeglimin Normalizes Glucose Tolerance and Insulin Sensitivity and Improves Mitochondrial Function in Liver of a High-Fat High-Sucrose Diet Mice Model. Diabetes. 2014. pii: db141220

 

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:Imeglimin hydrochloride 

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