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编 号:F516410
分子式:C18H19F8N5O2
分子量:489.36
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生物活性:
Gemigliptin (LC15-0444 ) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin exhibits potent anti-glycation properties. Gemigliptin can be used for the research of advanced glycation end products (AGE)-related diabetic complications.

体内研究:
Gemigliptin (100 mg/kg; i.g.; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo.Gemigliptin dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys.Animal Model:Male C57BL/KsJ-db/db mice (7 weeks old)
Dosage:100 mg/kg
Administration:Oral gavage, daily, for 12 weeks
Result:Significantly reduced circulating AGE levels by 44.5% in serum.

体外研究:
Gemigliptin dose-dependently inhibits the formation of AGE-BSA with IC50 of 11.69 mM.Gemigliptin dose-dependently suppressed the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50 of 1.39 mM.Gemigliptin is a competitive inhibitor with a Ki of 7.25 nM.
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