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| 描述 | α-glucosidases are enzymes responsible for the metabolism of complex carbohydrates into absorbable monosaccharide units. However, hyperglycemia causes a number of abnormalities which contribute to the development of long-term complications of diabetes. Acarbose, an anti-diabetic drug, is an intestinal α-glucosidase inhibitor[3]. In TNF-α pre-treated A7r5 cells, acarbose (1, 2, and 3 μM) dose-dependently decreased β-galactosidase, Ras expression and increased p-AMPK expression. In HCD (high cholesterol diet)-fed rabbits, the numbers of atherosclerotic plaques in the aortic arch were significantly decreased by acarbose treatment (2.5 and 5.0 mg/kg per day). Further, acarbose (2.5 and 5.0 mg/kg) significantly and dose-dependently decreased the intensity of neointimal IL-6, TNF-α, and iNOS staining, and significantly increased the intensity of neointimal p-AMPK staining. Moreover, acarbose (2.5 and 5.0 mg/kg) significantly and dose-dependently decreased neointimal Ras and β-galactosidase expression in HCD-fed rabbits[4]. |
| Concentration | Treated Time | Description | References | |
| Bone marrow-derived macrophages (BMDMs) | 250 μM | 48 h | To investigate the direct effects of Acarbose on the survival and proinflammatory function of M1-polarized macrophages. Results showed that Acarbose significantly increased apoptosis of M1-polarized macrophages and reduced TNF-α secretion. | Cell Rep Med. 2025 Jan 21;6(1):101883 |
| Bacteroides ovatus (Bo) | 25 µM | 144 h | To evaluate the effect of Acarbose on the growth of different Bacteroides species, it was found that Bo growth is much less affected. | mBio. 2024 Dec 11;15(12):e0150624 |
| Bacteroides thetaiotaomicron (Bt) | 25 µM | 144 h | To evaluate the effect of Acarbose on the growth of different Bacteroides species, it was found that Bt growth on starch polysaccharides is severely impaired. | mBio. 2024 Dec 11;15(12):e0150624 |
| Macrophages | 10.0 µg/mL | 48 h | Assess the therapeutic effect of Acarbose on L. infantum-infected macrophages, resulting in an 87.4% reduction in infectivity. | Med Microbiol Immunol. 2021 Jun;210(2-3):133-147 |
| L. infantum promastigotes | 0.47 ± 0.1 µg/mL (IC50) | 48 h | Evaluate the direct antileishmanial activity of Acarbose against L. infantum promastigotes, showing significant inhibitory effects. | Med Microbiol Immunol. 2021 Jun;210(2-3):133-147 |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Apc+/Min mouse model | Oral | 296 ppm and 935 ppm | Continuous feeding starting at 42 days of age | Acarbose improved the median survival of Apc+/Min mice, with low dose (296 ppm) and high dose (935 ppm) increasing survival by 15.2% and 21.4%, respectively. The high dose also reduced tumor number and improved hematocrit. | Aging Cell. 2020 Feb;19(2):e13088 |
| HET3 mice | Genetically heterogeneous mice | Dietary administration | 400, 1000, 2500 ppm | Continuous administration starting at 8 months of age | Acarbose significantly extended the lifespan of male mice with smaller effects in females. Higher doses of acarbose reduced lung tumors in males, diminished liver degeneration in both sexes and glomerulosclerosis in females, reduced blood glucose responses to refeeding in males, and improved rotarod performance in aging females, but not males. | Aging Cell. 2019 Apr;18(2):e12898 |
| Mice | UM-HET3 mice | Diet | 1000 ppm | Continuous administration starting from 4 months of age | To evaluate the effects of acarbose on lifespan. Results showed that acarbose significantly increased male median lifespan by 22% (P<0.0001), but only increased female median lifespan by 5% (P=0.01). Maximum lifespan (90th percentile) increased by 11% (P<0.001) in males and 9% (P=0.001) in females. | Aging Cell. 2014 Apr;13(2):273-82 |
| 3xTg and non-transgenic (NTg) mice | Alzheimer’s disease model | Dietary administration | 1000 ppm | Started at 6 months of age and continued for 6 months | Acarbose ameliorates Western diet-induced metabolic and cognitive impairments, reduces body weight and adiposity, increases energy expenditure, improves glycemic control, and reverses WD-induced cognitive deficits. | Geroscience. 2025 Apr;47(2):1569-1591 |
| C57BL/6J mice | High-fat diet-induced type 2 diabetic mouse model | Oral gavage | 40 mg/kg | Once daily for two weeks | To investigate the effect and mechanism of acarbose on Pseudomonas aeruginosa respiratory tract infection in T2DM and non-diabetic mice. Results showed that acarbose treatment significantly reduced mortality, alleviated lung inflammation, and decreased infection severity in both diabetic and non-diabetic mice. | Respir Res. 2023 Dec 14;24(1):312 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02476760 | - | Completed | - | Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 << | |
| NCT02475499 | - | Completed | - | Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 << | |
| NCT00000620 | Atherosclerosis ... 展开 >> Cardiovascular Diseases Hypercholesterolemia Hypertension Diabetes Mellitus, Type 2 Diabetes Mellitus Coronary Disease 收起 << | Phase 3 | Completed | - | United States, Minnesota ... 展开 >> Minneapolis Medical Research Foundation Minneapolis, Minnesota, United States, 55404 United States, New York Columbia University New York, New York, United States, 10027 United States, North Carolina Wake Forest University Winston-Salem, North Carolina, United States, 27106 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 United States, Tennessee Veterans Affairs Memphis, Tennessee, United States, 38104 United States, Washington University of Washington Seattle, Washington, United States, 98195 Canada, Ontario McMaster University Hamilton, Ontario, Canada 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.55mL 0.31mL 0.15mL |
7.74mL 1.55mL 0.77mL |
15.49mL 3.10mL 1.55mL |
|
| CAS号 | 56180-94-0 |
| 分子式 | C25H43NO18 |
| 分子量 | 645.6 |
| SMILES Code | O[C@H]1[C@]([H])(O[C@H]([C@@H]2O)O[C@@H]([C@H]([C@@H]2O)N[C@@]([H])(C=C3CO)[C@H](O)[C@H]([C@@H]3O)O)C)[C@@H](CO)O[C@@H]([C@@H]1O)O[C@@]([H])([C@@H]([C@H](C=O)O)O)[C@@H](CO)O |
| MDL No. | MFCD00869592 |
| 别名 | 阿卡波糖水合物 ;BAY g 5421 |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C |
| 溶解方案 |
H2O: 100 mg/mL(154.89 mM),配合低频超声助溶
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