Acarbose

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.
Targets
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]

Protocol

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
Formula

C25H43NO18

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02953093 Not yet recruiting Aging Montefiore Medical Center November 2016 Phase 2
NCT02836704 Recruiting Diabetes Mellitus, Type 2 Sanofi September 2016 Phase 4
NCT02879955 Recruiting Overweight Hvidovre University Hospital|University of Copenhagen August 2016 --
NCT02865499 Recruiting Aging The University of Texas Health Science Center at San Antonio June 2016 Phase 2
NCT02999841 Recruiting Diabetes Mellitus, Type 2|Obesity Peking University March 2016 Phase 4
NCT02685852 Recruiting Hyperinsulinemic Hypoglycemia University of Minnesota - Clinical and Translational Science Institute February 2016 Phase 2

Tech Support

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.

Handling Instructions

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