Acarbose

For research use only.

Catalog No.S1271 Synonyms: BAY g 5421

1 publication

Acarbose Chemical Structure

CAS No. 56180-94-0

Acarbose(BAY g 5421) is an inhibitor of intestinal alpha-glucosidase, used to treat type 2 diabetes mellitus.

Selleck's Acarbose has been cited by 1 publication

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Biological Activity

Description Acarbose(BAY g 5421) 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
in solvent
Synonyms BAY g 5421
Smiles CC1C(C(C(C(O1)OC2C(OC(C(C2O)O)OC3C(OC(C(C3O)O)O)CO)CO)O)O)NC4C=C(C(C(C4O)O)O)CO

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04665570 Recruiting Drug: BAY81-9783 (Acarbose/Metformin) Type 2 Diabetes Mellitus Bayer December 21 2020 --
NCT04180813 Recruiting Drug: Linagliptin|Drug: Acarbose Diabetes Mellitus Type 2 Boehringer Ingelheim March 4 2020 --
NCT02589353 Recruiting Drug: Acarbose Healthy Volunteers Oregon State University April 21 2017 Phase 4
NCT02953093 Completed Drug: Acarbose|Other: Placebo Aging Montefiore Medical Center November 22 2016 Phase 2
NCT02527239 Unknown status Other: Prospective observational study Pompe''s Disease Royal Brompton & Harefield NHS Foundation Trust|Genzyme a Sanofi Company September 2015 --
NCT01961388 Withdrawn Drug: Bay G5421 Glucobay|Drug: Metformin Diabetes Mellitus Bayer August 2015 --

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID