Acarbose

Acarbose 속성

Acarbose C화학적 특성, 용도, 생산

개요

Acarbose, a complex oligosaccharide isolated from Actinoplanes, is reportedly useful as an adjuvant therapy in diabetes. By inhibiting alpha-glucosidase, acarbose delays carbohydrate metabolism in the gastrointestinal tract and modulates changes in food induced blood sugar levels.

화학적 성질

Off-White Solid

용도

Acarbose is pseudo-oligosaccharide with a terminal C7-cyclitol patented in 1975 by Bayer. Acarbose is a component of the amylostatin complex produced by a species of Actinoplanes and Streptomyces. Acarbose acts as a potent inhibitor of alpha-glucosidases and saccharases. Since 1990, acarbose has been used therapeutically for the treatment of type 2 diabetes.

정의

ChEBI: A tetrasaccharide derivative consisting of a dideoxy-4-{[4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl C7 cyclitol moiety [called valienol (or valienamine)] linked via nitrogen to isomaltotriose.

World Health Organization (WHO)

Acarbose, ana-glucosidase inhibitor, is used as an adjunctive therapy in the control of postprandial hyperglycaemia in non-insulin-dependent diabetes mellitus. Use of two or more hypoglycaemic drugs is not recommended.

일반 설명

Acarbose is a naturally occurring oligosaccharide,which is obtained from the microorganism Actinoplanes utahensis. It is a white to off-white powder that is soluble in water and has a pKa of 5.1. As one mightexpect, its affinity for α-glucosidase is based on it being apolysaccharide that the enzyme attempts to hydrolyze. Thisallows acarbose to act as a competitive inhibitor, which inturn reduces the intestinal absorption of starch, dextrin, anddissacharides.
It is sold as 25-, 50-, and 100-mg tablets (Precose,generics) dosed with the first bite of each meal, up to t.i.d. Acarbose potently inhibits the glucoamylase activity of MGAM α-glucosidases and the sucrase activity of α-glucosidases, where as isomaltase activity is at most moderately inhibited at concentrations in the range of those in theintestinal lumen upon oral dosing, and trehalase and lactaseare not significantly inhibited. Some inhibition of pancreaticα-amylases may also contribute to the clinical effects.
https://www.sciencedirect.com

Clinical Use

Based on the structure of acarbose, it should come as nosurprise that little intact acarbose reaches the systemic circulation;instead, acarbose is extensively biotransformed by the actionof microbes and digestive enzymes in the gut. Only about35% of the radioactivity in a dose of ¹⁴C-labeled acarbose administeredorally to men was excreted in the urine, appearingas several metabolites, some of which are phase II conversionproducts of 4-methylpyrogallol (O-methyl, O-sulfate, orO-glucuronide conjugates); the methylpyrogallol fragmentarises from the terminal valienamine pseudosugar. That thesebiotransformation products are mostly formed in the gut isshown by the fact that nearly 90% of an intravenously administereddose of acarbose is excreted intact in urine.

Safety Profile

Low toxicity by ingestion,subcutaneous, and intravenous routes. Human systemiceffects: liver function impaired. When heated todecomposition it emits toxic vapors of NOx.

Acarbose 준비 용품 및 원자재

원자재

준비 용품

Acarbose 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Hebei Mojin Biotechnology Co., Ltd	+8613288715578	sales@hbmojin.com	China	12468	58
Changzhou Rokechem Technology Co., Ltd.	18758118018	sales001@rokechem.com	China	255	58
Hebei Jingbo New Material Technology Co., Ltd	+8619931165850	hbjbtech@163.com	China	1000	58
Henan Fengda Chemical Co., Ltd	+86-371-86557731 +86-13613820652	info@fdachem.com	China	18219	58
Sigma Audley	+86-18336680971 +86-18126314766	nova@sh-teruiop.com	China	525	58
Hebei Saisier Technology Co., LTD	+86-18400010335 +86-18034520335	admin@hbsaisier.cn	China	940	58
Shaanxi TNJONE Pharmaceutical Co., Ltd	+8618740459177	sarah@tnjone.com	China	1142	58
Hebei Longbang Technology Co., LTD	+86-18032476855 +86-18032476855	admin@hblongbang.com	China	902	58
Shanghai Daken Advanced Materials Co.,Ltd	+86-371-66670886	info@dakenam.com	China	15956	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21688	55

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