Acarbose (Synonyms: BAY-g 5421) |
| Katalog-Nr.GC10751 |
Alpha-Glucosidase-Inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 56180-94-0
Sample solution is provided at 25 µL, 10mM.
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.
| 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 | |
| Überlieferungen | BAY-g 5421 | ||
| Chemical Name | (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 | ||
| Formula | C25H43NO18 | M.Wt | 645.6 |
| Löslichkeit | ≥ 22.35mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5489 mL | 7.7447 mL | 15.4895 mL |
| 5 mM | 309.8 μL | 1.5489 mL | 3.0979 mL |
| 10 mM | 154.9 μL | 774.5 μL | 1.5489 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *