For research use only. Not for therapeutic Use.
Gemigliptin tartrate (LC15-0444 tartrate) 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 tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications[1][2].
Gemigliptin tartrate dose-dependently inhibits the formation of AGE-BSA with IC50 of 11.69 mM[1].
Gemigliptin tartrate dose-dependently suppresses the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50 of 1.39 mM[1].
Gemigliptin tartrate is a competitive DPP-4 inhibitor with a Ki of 7.25 nM[2].
Gemigliptin tartrate (100 mg/kg; i.g.; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo[1].
Gemigliptin tartrate dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys[2].
| Catalog Number | I045785 |
| CAS Number | 1374639-74-3 |
| Synonyms | 1-[(2S)-2-amino-4-[2,4-bis(trifluoromethyl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]-4-oxobutyl]-5,5-difluoropiperidin-2-one;(2R,3R)-2,3-dihydroxybutanedioic acid |
| Molecular Formula | C22H25F8N5O8 |
| Purity | ≥95% |
| InChI | InChI=1S/C18H19F8N5O2.C4H6O6/c19-16(20)3-1-12(32)31(8-16)6-9(27)5-13(33)30-4-2-10-11(7-30)28-15(18(24,25)26)29-14(10)17(21,22)23;5-1(3(7)8)2(6)4(9)10/h9H,1-8,27H2;1-2,5-6H,(H,7,8)(H,9,10)/t9-;1-,2-/m01/s1 |
| InChIKey | DPEZWSNXONTJHT-NDAAPVSOSA-N |
| SMILES | C1CC(CN(C1=O)CC(CC(=O)N2CCC3=C(C2)N=C(N=C3C(F)(F)F)C(F)(F)F)N)(F)F.C(C(C(=O)O)O)(C(=O)O)O |
| 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. |
