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Acarbose.

(Synonyms: 阿卡波糖; BAY g 5421)

目录号: PC14747 纯度: ≥98%

α-葡糖苷酶抑制剂，Acarbose 是α葡萄糖苷酶抑制剂，具有抗糖尿病的作用。

CAS No. :56180-94-0

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中文名称

Acarbose.

中文别名

阿卡波糖;卡(波)糖;阿卡玻糖;拜糖平;O-4,6-二脱氧-4-[[1S-(1Α,4Α,5Β,6Α-)-4,5,6-三羟基-3-羟甲基-2-环己烯-1-基]氨基]-Α-D-吡喃葡萄糖基-(1→4)-O-Α-D-吡喃葡萄糖基-(1→4)-D-葡萄糖;阿卡糖;阿卡波糖杂质;阿卡波糖水合物;Acarbose Hydrate 阿卡波糖水合物;Acarbose 阿卡波糖;Acarbose 阿卡波糖标准品;阿卡波糖 EP标准品;阿卡波糖 USP标准品;阿卡波糖(Acarbosum);阿卡波糖峰鉴别 EP标准品;阿卡波糖鉴别 EP标准品;O-4,6-双脱氧-4[[(1S,4R,5S,6S)4,5,6-三羟基-3-(羟基甲基)-2-环己烯]氨基]-(-D-吡喃葡糖基(1→4)-O-)-D-吡喃葡糖基(1→4)-D-吡喃葡萄糖;降糖药;抑葡萄糖苷酶;O-4,6-双脱氧-4[[(1S,4R,5S,6S)4,5,6-三羟基-3-(羟基甲基)-2-环己烯]氨基]-(-D-吡喃葡糖基(1→4)-O-)-D-吡喃葡糖基(1→4)-D-吡喃葡萄糖;舒更葡糖钠Org198786-1杂质阿卡波糖杂质

英文名称

Acarbose

英文别名

acarbose;bay-g5421;d-glucose,o-4,6-dideoxy-4-(((1s-(1-alpha,4-alpha,5-beta,6-alpha))-4,5,6-trihyd;roxy-3-(hydroxymethyl)-2-cyclohexen-1-yl)amino)-alpha-d-glucopyranosyl-(1-4)-o;5-[5-[3,4-DIHYDROXY-6-METHYL-5-[[4,5,6-TRIHYDROXY-3-(HYDROXYMETHYL)-1-CYCLOHEX-2-ENYL]AMINO]OXAN-2-YL]OXY-3,4-DIHYDROXY-6-(HYDROXYMETHYL)OXAN-2-YL]OXY-6-(HYDROXYMETHYL)OXANE-2,3,4-TRIOL;Glucobay;Acarbose Hydrate;O-4,6-DIDEOXY-4-[[[1S-(1A,4A,5BETA,6A)]-4,5,6-TRIHYDROXY-3-(HYDROXYMETHY;acarviostatin I01;Ascarbose;Prandase;Precos;Precose;4",6"-Dideoxy-4"-([1S]-[1,4,6/5]-4,5,6-trihydroxy-3-hydroxymethyl-2-yclohexenylamino)-maltotriose;Sugammadex sodium Impurity;acarbose iMpurity;Beta-Acarbose;XUFXOAAUWZOOIT-SXARVLRPSA-N;DSSTox_RID_81300;DSSTox_CID_26034;DSSTox_GSID_46034;Arcabose;Glucor;1agm;1ukt;QPS;Acarbose, >=95%;HMC-(1-4)AGL-(1-4)GLC-(1-4)GLC;GTPL6791;HMS3677P19;HMS3413P19;HMS3269L19;BCPP000442;HMS3713B18;Tox21_111597;s1271;BDBM50333465;Tox21_111597_1;AKO

Cas No.

56180-94-0

分子式

C₂₅H₄₃NO₁₈

分子量

645.60

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

详情描述

α-葡糖苷酶抑制剂，Acarbose 是α葡萄糖苷酶抑制剂，具有抗糖尿病的作用。

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.

性状

Solid

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.

Medlife 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.
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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

结构分类

来源

Actinoplanes sp

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. [Information]

[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. [Information]

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

[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. [Information]

[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 [Information]

溶解度数据

体外研究:

H₂O : 100 mg/mL (154.89 mM; Need ultrasonic)

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (154.89 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

搜索质检报告(COA)

产品使用指南

Data Sheet

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

[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. [Information]

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

[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. [Information]

[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 [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Acarbose.

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