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Vildagliptin

商品编号: TL0112
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详细介绍

l  基本信息

产品名称

维他列汀(Vildagliptin)

一般描述

Vildagliptin(维他列汀) is a cyanopyrrolidine-based, orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity.

别 称

(2S)-1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile; NVP-LAF 237;Galvus; Xiliarx; Jalra;

纯 度

≥99%(HPLC)

CAS NO.

274901-16-5

分子式

C17H25N3O2

分子量

303.406

适用范围

生物试剂,适用于细胞培养等

l  理化信息

外 观

白色至类白色固体

溶解性(25)

DMSO

≥50mg/mL

乙醇

≥50mg/mL

≥50mg/mL

l  生物学信息

生物活性/药理作用

Vildagliptin belongs to a class of orally active antidiabetic drugs (DPP-IV inhibitors) that appear to have multiple functional benefits beyond simple blood-glucose control. One of these is a potential protective effect on pancreatic beta cells, which deteriorate in  diabetes. Vildagliptin appears to be safe, very well tolerated, and  efficacious. Following a meal, gut incretin hormones are released. The most important incretin hormones are GLP-1 and glucose-dependent insulinotropic polypeptide (GIP). These hormones, secreted in the human small intestine, are responsible for insulin release due to increased glucose levels. In contrast  to agents that promote insulin secretion via glucose-independent mechanisms,  GLP-1's dependence on glucose concentration is considered beneficial due to a lower risk of hypoglycemia. GLP-1 also inhibits glucagon secretion and  increases beta cell mass by stimulating proliferation and neogenesis. However, the clinical utility of GLP-1 is limited by its short half-life (2  minutes). GLP-1 is rapidly degraded by the proteolytic enzyme DPP-IV. To enhance GLP-1 activity, inhibition of the DPP-IV enzyme is emerging as a novel therapeutic approach in the treatment of diabetes. Administration of vildagliptin enhances GLP-1's ability to produce insulin in response to elevated concentrations of blood glucose, inhibit the release of glucagon  following meals, slow the rate of nutrient absorption into the bloodstream,  slow the rate of gastric emptying, and reduce food intake.

l  包装与存储

包 装

250mg; 1g

存储温度

0-5

l  注意事项及免责声明

本产品仅用于实验研究,不得作为药物使用,不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.   https://www.ncbi.nlm.nih.gov