Acarbose(Synonyms: 阿卡波糖; BAY g 5421)

天然产物 糖类和糖苷 Saccharides and Glycosides

Acarbose;(Synonyms: 阿卡波糖; BAY g 5421) 纯度: ge;98.0%

Acarbose (BAY g 5421),降糖药,是一种具有口服活性 α-葡萄糖苷酶 (alpha-glucosidase) 抑制剂 (IC50=11 nM)。Acarbose 能增强磺脲类药物或胰岛素的降血糖作用。

Acarbose(Synonyms: 阿卡波糖; BAY g 5421)

Acarbose Chemical Structure

CAS No. : 56180-94-0

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生物活性

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[1][2][3].

体外研究
(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[5].

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

体内研究
(In Vivo)

Acarbose (300 mg/60 kg body weight) decreases the fasting blood glucose, and regulates the glucose tolerance of DM rats without body weight loss. Acarbose significantly suppresses serum IL6 and TNF-α in DM rats[4].
Acarbose (2.5 and 5.0 mg/kg) significantly and dose-dependently decreases the intensity of neointimal IL-6, TNF-α, and iNOS staining, and significantly increases the intensity of neointimal p-AMPK staining. Acarbose (2.5 and 5.0 mg/kg) significantly and dose-dependently decreases neointimal Ras and β-galactosidase expression in HCD-fed rabbits without body weight loss[5].

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

Clinical Trial

分子量

645.60

Formula

C25H43NO18

CAS 号

56180-94-0

中文名称

阿卡波糖

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20deg;C 3 years
4deg;C 2 years
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

H2O : 125 mg/mL (193.62 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5489 mL 7.7447 mL 15.4895 mL
5 mM 0.3098 mL 1.5489 mL 3.0979 mL
10 mM 0.1549 mL 0.7745 mL 1.5489 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [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

Cell Assay
[2]

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 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [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

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