α-Glucosidase-IN-98
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.
For research use only. We do not sell to patients.
- Formula: C19H19NO3
- Molecular Weight:309.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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α‑glucosidase 18.1 μM (IC50) |
α-Glucosidase-IN-98 (compound 5c) maintains strong α-Glucosidase inhibitory activity in the presence of polysaccharides (Acacia gum (HY-N6664), Pectin (HY-W145518)), unlike with proteins, fatty acids, or PEG, which cause significant attenuation[1].
α-Glucosidase-IN-98 (0-40 μM) reversibly inhibits α-Glucosidase via non-covalent interactions, exhibiting a higher binding affinity for the enzyme-substrate complex (Ki = 13.9 μM) than for the free enzyme (Ki = 42.2 μM)[1].
α-Glucosidase-IN-98 binds with α-Glucosidase mainly through hydrogen bonds (with Asp69, Asp352, His280), electrostatic interactions (with Asp215, Asp315), and hydrophobic interactions (with Val216), consistent with the static quenching[1].
α-Glucosidase-IN-98 (0-46.4 μM) reduces the surface hydrophobicity of α-Glucosidase by 29.4%, and induces a structural shift (decreased α-helix, increased β-sheet) that enhances rigidity, suggesting that it can stabilize the enzyme by occupying the hydrophobic cavity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Kunming mice (7 weeks) with postprandial hyperglycemia induced by acute high-dose (3 g/kg) starch administration[1]
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Dosage:10, 20 and 40 mg/kg
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Administration:p.o., single dose
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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.
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Animal Model:Male Kunming mice (7 weeks) with postprandial hyperglycemia induced by acute high-dose (3 g/kg) sucrose administration[1]
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Dosage:10, 20 and 40 mg/kg
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Administration:p.o., single dose
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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.
Chemical Information
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Molecular Weight 309.36
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Formula C19H19NO3
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SMILES
COC1=CC(CCC(CCC2=CC=C(C=C2)C#N)=O)=CC=C1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
α-Glucosidase-IN-98 Related Classifications
HY-178383 Related Classifications
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