| Bioactivity | 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[1][2]. |
| Target | IC50: 10.3 nM (human recombinant DPP-4) |
| Invitro | Gemigliptin dose-dependently inhibits the formation of AGE-BSA with IC50 of 11.69 mM[1].Gemigliptin dose-dependently suppressed the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50 of 1.39 mM[1].Gemigliptin is a competitive inhibitor with a Ki of 7.25 nM[2]. |
| In Vivo | Gemigliptin (100 mg/kg; i.g.; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo[1].Gemigliptin dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys[2]. Animal Model: |
| Name | Gemigliptin |
| CAS | 911637-19-9 |
| Formula | C18H19F8N5O2 |
| Molar Mass | 489.36 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Jung E, et al. Gemigliptin, a novel dipeptidyl peptidase-4 inhibitor, exhibits potent anti-glycation properties in vitro and in vivo. Eur J Pharmacol. 2014 Dec 5;744:98-102. [2]. Kim SH, et al. Pharmacological profiles of gemigliptin (LC15-0444), a novel dipeptidyl peptidase-4 inhibitor, in vitro and in vivo. Eur J Pharmacol. 2016 Oct 5;788:54-64. |