α-Glucosidase-IN-57

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α-Glucosidase-IN-57 (Compound 10c) is a competitive and orally active α-glucosidase inhibitor with an IC₅₀ value of 0.180 μM and a K_i of 0.15 μM. α-Glucosidase-IN-57 can reduce fasting and overall blood glucose levels in mice, and can be used for anti-diabetes research.

For research use only. We do not sell to patients.

α-Glucosidase-IN-57 Chemical Structure

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Biological Activity
Purity & Documentation
References
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Description

In Vitro

α-Glucosidase-in-57 (Compound 10c) (0, 0.045, 0.09, 0.18 μM) competes with the substrate p-NPG (HY-W039892) (1-16 μM) for the same active site of the α-Glucosidase enzyme. α-Glucosidase-IN-57 acts as a potent competitive inhibitor of alpha-glucosidase^[1].

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

In Vivo

α-Glucosidase-IN-57 (Compound 10c) (250, 500, 1000 mg/kg; Oral gavage (p.o.); 72h) is well tolerated and safe in Wistar albino rat models^[1].
α-Glucosidase-IN-57 (10, 25, 50 mg/kg; Oral gavage (p.o.); once daily for 28 days) has hypoglycemic activity in a Wistar albino rat model of diabetes, including reduces fasting blood glucose levels, improves glucose tolerance, and possibly improves islet structure of pancreatic tissue^[1].

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

Animal Model:	Male Wistar albino rats with diabetes^[1]
Dosage:	α-Glucosidase-IN-57: 10, 25, 50 mg/kg; Acarbose: 50 mg/kg
Administration:	Oral gavage (p.o.); once daily for 28 days
Result:	In the first 7 days, fasting blood glucose levels were not significantly different from diabetic controls. On day 14, significantly reduced blood glucose levels at oral doses of 25 and 50 mg/kg, while Acarbose (at oral doses of 50 mg/kg) achieved the same effect. On day 21, had the best hypoglycemic effect with acarbose at oral doses of 25 and 50 mg/kg, which was significantly better than the diabetic control group. On day 28, blood glucose levels were significantly lower than those in the diabetic control group.

Molecular Weight

530.61

Formula

C₃₂H₂₃FN₄OS

SMILES

O=C(CSC1=NC2=CC=CC=C2C=C1C3=NC(C4=CC=CC=C4)=C(N3)C5=CC=CC=C5)NC6=CC=C(F)C=C6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Khalili Ghomi M, et al. Evaluation of novel 2-(quinoline-2-ylthio)acetamide derivatives linked to diphenyl-imidazole as α-glucosidase inhibitors: Insights from in silico, in vitro, and in vivo studies on their anti-diabetic properties. Eur J Med Chem. 2024 Apr 5;269:116332. [Content Brief]