Acarbose [56180-94-0]

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Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin.

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Acarbose Chemical Structure

CAS No. : 56180-94-0

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  • Pest Manag Sci. 2021 Jul 26.  [Abstract]
  • Phytochemistry. 2022 Jan 6;196:113083.  [Abstract]
  • Nat Prod Bioprospect. 2023 Jan 9;13(1):2.  [Abstract]
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Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin.

In Vitro

Acarbose (1, 2, and 3 μM) dose- and time-dependently inhibits TNF-α-induced VSMC proliferation and migration. Acarbose (1, 2, and 3 μM) dose-dependently decreases β-galactosidase, Ras expression and increased p-AMPK expression in TNF-α pre-treated A7r5 cells.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

  • [1]. Yee HS, et al. A review of the safety and efficacy of acarbose in diabetes mellitus. Pharmacotherapy. 1996;16(5):792-805.  [Content Brief]

    [2]. Hanefeld M, et al. Acarbose: oral anti-diabetes drug with additional cardiovascular benefits [published correction appears in Expert Rev Cardiovasc Ther. 2009 Mar;7(3):330]. Expert Rev Cardiovasc Ther. 2008;6(2):153-163.  [Content Brief]

    [3]. Oki T, et al. Evaluation of alpha-glucosidase inhibition by using an immobilized assay system. Biol Pharm Bull. 2000;23(9):1084-1087.  [Content Brief]

    [4]. Zhang Q, et al. Acarbose Reduces Blood Glucose by Activating miR-10a-5p and miR-664 in Diabetic Rats. PLoS One. 2013 Nov 18;8(11):e79697.  [Content Brief]

    [5]. Chan KC, et al. Pleiotropic effects of acarbose on atherosclerosis development in rabbits are mediated via upregulating AMPK signals. Sci Rep. 2016 Dec 7;6:3864  [Content Brief]

Cell viability is determined using the MTT assay. Cells are seeded in 24-well culture plates at a density of 2×104 cells/well, incubated for 48 h, treated with acarbose at varying concentrations (0.5, 1.0, 2.0, 3.0, and 5.0 μM) for 24 h; or pre-treated with TNF-α (20 ng/mL) for either 24 h or 48 h to evaluate the dose-dependent effects of acarbose on VSMC growth and viability, cultured with 0.5 mg/mL MTT at 37°C in a humidified atmosphere of 5% CO2 for another 4 h, and solubilized with isopropanol. The viable cell number varies directly with the concentration of formazan product measured spectrophotometrically at 563 nm.

MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

Twenty-four male New Zealand white rabbits, weighing 2500 g are used. They are individually housed in metal cages in an air-conditioned room (22 ± 2°C, 55 ± 5% humidity), under a 12 h light/12 h dark cycle with free access to food and water. All rabbits are randomLy assigned to four groups of 6 animals each and are fed either standard chow (Group I), high cholesterol diet (HCD; containing 95.7% standard Purina chow + 3% lard oil + 0.5% cholesterol) (Group II), HCD diet and 2.5 mg/kg per day acarbose (Group III), or HCD diet and 5.0 mg/kg per day acarbose (Group IV). At the end of the 25 weeks, all rabbits are sacrificed by exsanguination under deep anesthesia with pentobarbital (30 mg/kg i.v.) injected via the marginal ear vein. Serum is stored at −80°C prior to measurement of serum values. The aortic arch and thoracic aortas are carefully removed to protect the endothelial lining, and are collected and freed of adhering soft tissue.

MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

  • [1]. Yee HS, et al. A review of the safety and efficacy of acarbose in diabetes mellitus. Pharmacotherapy. 1996;16(5):792-805.  [Content Brief]

    [2]. Hanefeld M, et al. Acarbose: oral anti-diabetes drug with additional cardiovascular benefits [published correction appears in Expert Rev Cardiovasc Ther. 2009 Mar;7(3):330]. Expert Rev Cardiovasc Ther. 2008;6(2):153-163.  [Content Brief]

    [3]. Oki T, et al. Evaluation of alpha-glucosidase inhibition by using an immobilized assay system. Biol Pharm Bull. 2000;23(9):1084-1087.  [Content Brief]

    [4]. Zhang Q, et al. Acarbose Reduces Blood Glucose by Activating miR-10a-5p and miR-664 in Diabetic Rats. PLoS One. 2013 Nov 18;8(11):e79697.  [Content Brief]

    [5]. Chan KC, et al. Pleiotropic effects of acarbose on atherosclerosis development in rabbits are mediated via upregulating AMPK signals. Sci Rep. 2016 Dec 7;6:3864  [Content Brief]

  • [1]. Yee HS, et al. A review of the safety and efficacy of acarbose in diabetes mellitus. Pharmacotherapy. 1996;16(5):792-805.

    [2]. Hanefeld M, et al. Acarbose: oral anti-diabetes drug with additional cardiovascular benefits [published correction appears in Expert Rev Cardiovasc Ther. 2009 Mar;7(3):330]. Expert Rev Cardiovasc Ther. 2008;6(2):153-163.

    [3]. Oki T, et al. Evaluation of alpha-glucosidase inhibition by using an immobilized assay system. Biol Pharm Bull. 2000;23(9):1084-1087.

    [4]. Zhang Q, et al. Acarbose Reduces Blood Glucose by Activating miR-10a-5p and miR-664 in Diabetic Rats. PLoS One. 2013 Nov 18;8(11):e79697.

    [5]. Chan KC, et al. Pleiotropic effects of acarbose on atherosclerosis development in rabbits are mediated via upregulating AMPK signals. Sci Rep. 2016 Dec 7;6:3864

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.5489 mL 7.7447 mL 15.4895 mL 38.7237 mL
5 mM 0.3098 mL 1.5489 mL 3.0979 mL 7.7447 mL
10 mM 0.1549 mL 0.7745 mL 1.5489 mL 3.8724 mL
15 mM 0.1033 mL 0.5163 mL 1.0326 mL 2.5816 mL
20 mM 0.0774 mL 0.3872 mL 0.7745 mL 1.9362 mL
25 mM 0.0620 mL 0.3098 mL 0.6196 mL 1.5489 mL
30 mM 0.0516 mL 0.2582 mL 0.5163 mL 1.2908 mL
40 mM 0.0387 mL 0.1936 mL 0.3872 mL 0.9681 mL
50 mM 0.0310 mL 0.1549 mL 0.3098 mL 0.7745 mL
60 mM 0.0258 mL 0.1291 mL 0.2582 mL 0.6454 mL
80 mM 0.0194 mL 0.0968 mL 0.1936 mL 0.4840 mL
100 mM 0.0155 mL 0.0774 mL 0.1549 mL 0.3872 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Metabolic Enzyme/Protease
  • Glucosidase
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Keywords:

Acarbose56180-94-0BAY g 5421BAY g5421BAY g-5421Glucosidaseantihyperglycemicanti-diabetesinsulinoralmellitusInhibitorinhibitorinhibit

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