Acarbose
(Synonyms: 阿卡波糖; BAY g 5421) 目录号 : GC10751
Acarbose是一种口服α-葡萄糖苷酶抑制剂（IC50 = 11nM），属于寡糖类药物。
Cas No.:56180-94-0
Sample solution is provided at 25 µL, 10mM.
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Acarbose is an oral α-glucosidase inhibitor (IC50 = 11nM), which belongs to the class of oligosaccharide drugs [1]. Acarbose mainly competitively and reversibly inhibits α-glucosidase and pancreatic amylase on the “brush border” of the small intestine, thereby delaying the decomposition of carbohydrates into monosaccharides and slowing down the rapid increase in blood sugar after meals [2-3]. Acarbose is mainly used as an adjuvant treatment for type 2 diabetes [4].
In A7r5 cells, Acarbose (0.5-5μM; 24h, 48h) inhibited the phosphorylation of focal adhesion kinase (FAK) and Akt, activities of the matrix metalloproteinases (MMPs) MMP-2 and MMP-9, and protein expressions of small G proteins (Ras, Cdc42, RhoA, and Rac1) in a dose-dependent manner [5]. In LPS-stimulated THP-1 cells, Acarbose (1μM; 24h) suppressed LPS-induced acetylation of histones H3 (H3) and H4 in the IP-10 and MCP-1 promoter regions [6]. In A7r5 cells, Acarbose (3μM; 24h) reduced diabetes-induced cell migration [7].
In streptozotocin-induced diabetic mice model, Acarbose (50mg/kg; po; 14d) administration by gavage reduced the severity of insulitis and improved insulin levels in the experimental diabetic mice [8]. In aging HET3 mice, Acarbose (1000mg/kg; po; 1200d) improves health and lifespan [9].
References:
[1]. Hanefeld M, Schaper F. Acarbose: oral antidiabetes drug with additional cardiovascular benefits[J]. Expert review of cardiovascular therapy, 2008, 6(2): 153-163.
[2]. Khan F, Khan M V, Kumar A, et al. Recent advances in the development of alpha-glucosidase and alpha-amylase inhibitors in type 2 diabetes management: insights from in silico to in vitro studies[J]. Current Drug Targets, 2024, 25(12): 782-795.
[3]. Bhatnagar A, Mishra A. α-Glucosidase inhibitors for diabetes/blood sugar regulation[M]//Natural products as enzyme inhibitors: An industrial perspective. Singapore: Springer Nature Singapore, 2022: 269-283.
[4]. Chiasson J L, Josse R G, Gomis R, et al. Acarbose for prevention of type 2 diabetes mellitus: the STOP-NIDDM randomised trial[J]. The Lancet, 2002, 359(9323): 2072-2077.
[5]. Yu M H, Lin M C, Huang C N, et al. Acarbose inhibits the proliferation and migration of vascular smooth muscle cells via targeting Ras signaling[J]. Vascular Pharmacology, 2018, 103: 8-15.
[6]. Lin Y C, Chen Y C, Hsiao H P, et al. The effects of acarbose on chemokine and cytokine production in human monocytic THP-1 cells[J]. Hormones, 2019, 18(2): 179-187.
[7]. Chuang W Y, Yu M H, Yang T Y, et al. Acarbose attenuates migration/proliferation via targeting microRNA-143 in vascular smooth muscle cells under diabetic conditions[J]. Journal of Food and Drug Analysis, 2020, 28(3): 461.
[8]. Zhao B, Wu F, Han X, et al. Protective effects of acarbose against insulitis in multiple low-dose streptozotocin-induced diabetic mice[J]. Life Sciences, 2020, 263: 118490.
[9]. Harrison D E, Strong R, Alavez S, et al. Acarbose improves health and lifespan in aging HET3 mice[J]. Aging cell, 2019, 18(2): e12898.
Acarbose是一种口服α-葡萄糖苷酶抑制剂（IC50 = 11nM），属于寡糖类药物 [1]。Acarbose主要竞争性地可逆性地抑制小肠“刷状缘”上的α-葡萄糖苷酶和胰淀粉酶，从而延缓碳水化合物分解为单糖，减缓餐后血糖的快速升高 [2-3]。Acarbose主要用于2型糖尿病的辅助治疗 [4]。
在A7r5细胞中，Acarbose（0.5-5μM；24h，48h）以剂量依赖性方式抑制黏着斑激酶（FAK）和Akt的磷酸化、基质金属蛋白酶（MMPs）MMP-2和MMP-9的活性以及小G蛋白（Ras、Cdc42、RhoA和Rac1）的蛋白表达 [5]。在LPS刺激的THP-1细胞中，Acarbose（1μM；24h）可抑制LPS诱导的IP-10和MCP-1启动子区组蛋白H3（H3）和H4的乙酰化 [6]。在A7r5细胞中，Acarbose（3μM；24h）可降低糖尿病诱导的细胞迁移 [7]。
在链脲佐菌素诱发的糖尿病小鼠模型中，通过管饲法给予Acarbose（50mg/kg；po；14d）可减轻实验性糖尿病小鼠的胰岛炎严重程度，并改善其胰岛素水平 [8]。在衰老的HET3小鼠中，Acarbose（1000mg/kg；po；1200d）可改善其健康和寿命 [9]。
| Cell experiment [1]: | |
Cell lines | A7r5 cells |
Preparation Method | A7r5 cells were seeded at a density of 2 × 105 cells/well into a 24-well plate and treated with Acarbose at various concentrations (0.5, 1.0, 2.0, 3.0, and 5.0μM) for either 24h or 48h. The cells were then treated with 0.5mg/mL MTT reagent at 37℃ in a humidified atmosphere of 5% CO2 for another 4h. |
Reaction Conditions | 0.5-5μM; 24h, 48h |
Applications | Acarbose inhibited the phosphorylation of focal adhesion kinase (FAK) and Akt, activities of the matrix metalloproteinases (MMPs) MMP-2 and MMP-9, and protein expressions of small G proteins (Ras, Cdc42, RhoA, and Rac1) in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Streptozotocin-induced diabetic mice model |
Preparation Method | Mice were administered with multiple low dose streptozotocin (STZ; 40mg/kg/day) for five consecutive days. Mice were randomly divided into three groups: the Control, STZ, and STZ + Acabose groups. The mice were administered vehicle solution of 0.1mM sodium citrate buffer (pH 4.5) were considered as the control. On the second day after the initial STZ injection, mice in the three groups were either treated with vehicle (0.5% carboxymethylcellulose, CMC) or Acarbose (50mg/kg/day for 14 days) by gavage. |
Dosage form | 50mg/kg; po; 14d |
Applications | Acarbose administration by gavage reduced the severity of insulitis and improved insulin levels in the experimental diabetic mice. |
References: | |
| Cas No. | 56180-94-0 | SDF | |
| 别名 | 阿卡波糖; BAY g 5421 | ||
| 化学名 | (3R,4R,5S,6R)-5-[(2R,3R,4R,5S,6R)-5-[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl]amino]oxan-2-yl]oxy-3,4-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-(hydroxymethyl)oxane-2,3,4-triol | ||
| Canonical 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 | ||
| 分子式 | C25H43NO18 | 分子量 | 645.6 |
| 溶解度 | ≥ 22.35mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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