α-Glucosidase-IN-11

α-Glucosidase-IN-11 is a highly permeable competitive α-glucosidase inhibitor with the IC50 value of 0.56 μM. α-Glucosidase-IN-11 binds to Trp residues in α-glucosidase and regulates protein folding. α-Glucosidase-IN-11 can be used to regulate blood glucose levels[1].

Research Areas >> Metabolic Disease

α-Glucosidase-IN-11 (compound 3k) inhibits α-glucosidase, α-fucosidase and α-mannosidase with the IC50 value of 0.56 μM, 30.4 μM and 41.2 μM, respectively[1]. α-Glucosidase-IN-11 (compound 3k) ( 0.1-100 μM, 24 hours) can induce β-cell proliferation at lower concentration[1]. Cell Proliferation Assay[1] Cell Line: BRIN-BD11 cells (rat beta cell line) Concentration: 0.1-100 μM Incubation Time: 24 hours Result: Showed cell proliferation at low concentration of 1 μM and minor cytotoxic effect at higher concentration greater than 10 μM.

α-Glucosidase-IN-11 (compound 3k) (gastric gavage, 60 mg/kg, everyday, 4 weeks) can improve blood glucose levels during fasting[1]. Animal Model: Male Sprague Dawley rats (250e320g)[1] Dosage: 60 mg/kg Administration: Gastric gavage; everyday; 4 weeks Result: Caused a significant drop in fasting blood glucose during the first and second weeks but did not cause a decrease in non-fasting blood glucose for up to four weeks.

[1]. Tania Luthra, et al. Discovery of novel pyrido-pyrrolidine hybrid compounds as alpha-glucosidase inhibitors and alternative agent for control of type 1 diabetes. Eur J Med Chem. 2020 Feb 15;188:112034.