Catalog No.S1271 Synonyms: BAY g 5421

Acarbose Chemical Structure

Molecular Weight(MW): 645.6

Acarbose is an inhibitor of intestinal alpha-glucosidase, used to treat type 2 diabetes mellitus.

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Biological Activity

Description Acarbose is an inhibitor of intestinal alpha-glucosidase, used to treat type 2 diabetes mellitus.
alpha-glucosidase [1]
In vitro

Acarbose reversibly inhibits intestinal alpha-glucosidases, enzymes responsible for the metabolism of complex carbohydrates into absorbable monosaccharide units.[1]

In vivo Acarbose reduces the absorption of monosaccharides derived from dietary carbohydrates, which play an important role in the metabolism and toxicity of some chemical compounds. Acarbose alone potentiates carbon tetrachloride (CCl4) andacetaminophen (AP) hepatotoxicity, as evidenced by significantly increased levels of both alanine transaminase (ALT) and aspartate transaminase (AST) in the plasma of rats pretreated with acarbose. [2] Acarbose treatment suppresses weight gain and the development of hepatic steatosis in sqstm1 gene knockout mice. Acarbose treatment up-regulates hepatic expression of the pparalpha, ucp-2, and abca1 genes, as well as srebp1c, pparalpha, and ppargamma in adipose tissue. [3] Acarbose-treated rats have lower body weights at 3 months of age with unaltered food consumption, and a similar effect is seen with a high-fructose diet in the JCR:LA-corpulent rat. [4] Acarbose markedly improves postprandial hyperglycemia, postprandial insulin level, total cholesterol, triglyceride, and free fatty acid level in Goto-Kakizaki (GK) rats. Acarbose efficiently reduces the number of monocytes adherent to aortic endothelial layer, improves acetylcholine-dependent vasodilatation, and reduces intimal thickening of the aorta in GK rats. [5]


Solubility (25°C)

In vitro DMSO 100 mg/mL (154.89 mM)
Water 100 mg/mL (154.89 mM)
Ethanol 8 mg/mL (12.39 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 645.6


CAS No. 56180-94-0
Storage powder
in solvent
Synonyms BAY g 5421

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02836704 Completed Diabetes Mellitus Type 2 Sanofi September 9 2016 Phase 4
NCT01709305 Completed Type 2 Diabetes Mellitus Merck Sharp & Dohme Corp. November 8 2012 Phase 4
NCT03349684 Recruiting Diabetes Mellitus Type 2 Bayer March 5 2018 Phase 3
NCT02315495 Completed Type 2 Diabetes Zilin Sun|Zhongda Hospital April 3 2015 Phase 3
NCT01177384 Completed Type 2 Diabetes Mellitus Merck Sharp & Dohme Corp. January 25 2011 Phase 3
NCT02953093 Recruiting Aging Montefiore Medical Center November 22 2016 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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