2. Metabolic Enzyme/Protease
  3. Glycosidase
  4. α-Glucosidase-IN-98

α-Glucosidase-IN-98 是一种强效的口服活性 α- 葡萄糖苷酶 (α-Glucosidase) 抑制剂，其 IC50 值为 18.1 μM。α-Glucosidase-IN-98 通过氢键、静电相互作用和疏水作用与 α- 葡萄糖苷酶可逆地结合，从而诱导酶二级结构发生显著的构象改变。α-Glucosidase-IN-98 能够降低淀粉 (HY-B2225B)/蔗糖 (HY-B1779) 负荷小鼠的餐后血糖水平。α-Glucosidase-IN-98 可用于 2 型糖尿病 (T2DM) 的相关研究。

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α-Glucosidase-IN-98

α-Glucosidase-IN-98 Chemical Structure

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α-Glucosidase-IN-98 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

α-Glucosidase-IN-98 is a potent orally active α-Glucosidase inhibitor with an IC50 of 18.1 μM. α-Glucosidase-IN-98 reversibly binds with α-Glucosidase via hydrogen bonds, electrostatic interactions and hydrophobic effects, which induces significant conformational alterations in the secondary structure of α-Glucosidase. α-Glucosidase-IN-98 decreases postprandial hyperglycemia in Starch (HY-B2225B)/Sucrose (HY-B1779)-challenged mice. α-Glucosidase-IN-98 can be used for type 2 diabetes mellitus (T2DM) research[1].

IC50 & Target[1]

α‑glucosidase

18.1 μM (IC50)

体外研究
(In Vitro)

α-Glucosidase-IN-98 (compound 5c) 在多糖 (Acacia gum (HY-N6664)、Pectin (HY-W145518)) 存在下能保持强效的 α- 葡萄糖苷酶抑制活性，这与在蛋白质、脂肪酸或 PEG 环境中其活性显著减弱的情况形成鲜明对比[1]。
α-Glucosidase-IN-98 (0-40 μM) 通过非共价相互作用可逆地抑制 α- 葡萄糖苷酶，并且对酶-底物复合物 (Ki = 13.9 μM) 的结合亲和力高于对游离酶 (Ki = 42.2 μM)[1]。
α-Glucosidase-IN-98 与 α- 葡萄糖苷酶的结合主要通过氢键 (与 Asp69、Asp352、His280)、静电相互作用 (与 Asp215、Asp315) 以及疏水作用 (与 Val216) 实现，这与静态猝灭的结果一致[1]。
α-Glucosidase-IN-98 (0-46.4 μM) 使 α- 葡萄糖苷酶的表面疏水性降低 29.4%，并诱导其发生 α- 螺旋减少、β- 折叠增加的结构转变，从而增强其刚性，这表明其可通过占据酶的疏水空腔来稳定其结构[1]。

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

α-Glucosidase-IN-98 相关抗体:
体内研究
(In Vivo)

α-Glucosidase-IN-98 (10、20 和 40 mg/kg，口服，单次给药) 在淀粉/蔗糖负荷小鼠中剂量依赖性地缓解餐后高血糖[1]。

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

Animal Model: Male Kunming mice (7 weeks) with postprandial hyperglycemia induced by acute high-dose (3 g/kg) starch administration[1]
Dosage: 10, 20 and 40 mg/kg
Administration: p.o., single dose
Result: Showed dose-dependent hypoglycemic effects.
Demonstrated progressively reduction in glycemic AUCs by 23.4%, 25.7%, and 29.4%, at 10, 20 and 40 mg/kg, respectively.
Resulted in lower blood glucose curves than the control group, demonstrating a notable delay in carbohydrate breakdown and absorption.
Animal Model: Male Kunming mice (7 weeks) with postprandial hyperglycemia induced by acute high-dose (3 g/kg) sucrose administration[1]
Dosage: 10, 20 and 40 mg/kg
Administration: p.o., single dose
Result: Displayed a dose-dependent decrease in AUC, with reductions of 10.5%, 15.8%, and 21.7%, at 10, 20, and 40 mg/kg, respectively.
Alleviated sucrose-induced postprandial hyperglycemia via α-Glucosidase inhibition.
分子量

309.36

Formula

C19H19NO3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

α-Glucosidase-IN-98 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

α-Glucosidase-IN-98Glycosidaseα-Glucosidasepostprandial hyperglycemiastarch/sucrose-challenged miceT2DMInhibitorinhibitorinhibit

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