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化合物简介

Acarbose is an anti-diabetic drug used to treat type 2 diabetes mellitus and, in some countries, prediabetes. It is a generic sold in Europe and China as Glucobay (Bayer AG), in North America as Precose (Bayer Pharmaceuticals), and in Canada as Prandase (Bayer AG). It is cheap and popular in China, but not in the U.S. One physician explains the use in the U.S. is limited because it is not potent enough to justify the side effects of diarrhea and flatulence. However, a recent large study concludes \"acarbose is effective, safe and well tolerated in a large cohort of Asian patients with type 2 diabetes.\" A possible explanation for the differing opinions is an observation that acarbose is significantly more effective in patients eating a relatively high carbohydrate Eastern diet ; It is a starch blocker, and inhibits alpha glucosidase, an intestinal enzyme that releases glucose from larger carbohydrates. It is composed of an acarviosin moiety with a maltose at the reducing terminus.

基本信息

CAS:56180-94-0
中文别名:阿卡波糖水合物;阿卡糖;
英文别名:bay-g5421;Ascarbose;Prandase;Glucobay;Acarbose;acarviostatin I01;Precose;Precos;
分子式:C25H43NO18
分子量:645.605
精确质量:645.248
Psa:321.17
Logp:-8.1736

编号系统

UNII:T58MSI464G

物化性质

外观与性状:灰白色固体
密度:1.74 g/cm3
沸点:971.6ºC at 760 mmHg
熔点:165-170ºC
闪点:541.4ºC
折射率:1.689
储存条件:库房通风低温干燥

安全信息

生产方法及用途

生产方法
从Axtinoplanes sp.SN 223/29发酵得到。 阿卡波糖是一种新型口服降糖药。在肠道内竞争性抑制葡萄糖甙水解酶。降低多糖及蔗糖分解成葡萄糖,使糖的吸收相应减缓,因此可具有使饭后血糖降低的作用。一般单用,或与其它口服降血糖药,或胰岛素合用。配合餐饮,治疗胰岛素依赖型或非依赖型糖尿病。
用途
阿卡波糖是一种新型口服降糖药。在肠道内竞争性抑制葡萄糖甙水解酶。降低多糖及蔗糖分解成葡萄糖,使糖的吸收相应减缓,因此可具有使饭后血糖降低的作用。一般单用,或与其它口服降血糖药,或胰岛素合用。配合餐饮,治疗胰岛素依赖型或非依赖型糖尿病。

合成路线

上游原料

下游产品

图谱

Predict 1H proton NMR


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