In Vitro: Gemigliptin tartrate dose-dependently inhibits the formation of AGE-BSA with IC50 of 11.69 mM. Gemigliptin tartrate dose-dependently suppresses the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50 of 1.39 mM. Gemigliptin tartrate is a competitive DPP-4 inhibitor with a Ki of 7.25 nM.
In Vivo: Gemigliptin tartrate (100 mg/kg; i.g.; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo. Gemigliptin tartrate dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys.