Gemigliptin

Gemigliptin (LC15-0444), is an oral anti-hyperglycemic agent (anti-diabetic drug). Currently, gemigliptin has been approved in 11 countries such as India, Columbia, Costa Rica, Panama, and Ecuador, and several clinical studies are in progress in Russia, Mexico, and Thailand.

General

Type : Drug,Piperidine,Pyrimidine,Gliptin,Trifluoro

Chemical_Nomenclature : 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

Canonical 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

InChI : InChI=1S\/C18H19F8N5O2\/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\/h9H,1-8,27H2\/t9-\/m0\/s1

InChIKey : ZWPRRQZNBDYKLH-VIFPVBQESA-N

Other name(s) : UNII-5DHU18M5D6,LC15-0444,(S)-1-(2-Amino-4-(2,4-bis(trifluoromethyl)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-4-oxobutyl)-5,5-difluoropiperidin-2-one,AK170799


MW : 489.37

Formula : C18H19F8N5O2

CAS_number : 911637-19-9

PubChem : 11953153

UniChem : ZWPRRQZNBDYKLH-VIFPVBQESA-N

IUPHAR :

Wikipedia : Gemigliptin

Target

Families : Gemigliptin ligand of proteins in family: DPP4N_Peptidase_S9

Stucture :

Protein : human-DPP4

References (8)

Title : Gemigliptin, a potent selective dipeptidyl peptidase 4 inhibitor, protects endothelial progenitor cells by oxidative stress via caspase-3 dependent pathway - Lee_2024_Biochem.Biophys.Rep_38_101673
Author(s) : Lee M , Tariq AR , Kim M
Ref : Biochem Biophys Rep , 38 :101673 , 2024
Abstract : Lee_2024_Biochem.Biophys.Rep_38_101673
ESTHER : Lee_2024_Biochem.Biophys.Rep_38_101673
PubMedSearch : Lee_2024_Biochem.Biophys.Rep_38_101673
PubMedID: 38444735

Title : Gemigliptin, a DPP4 inhibitor, ameliorates nonalcoholic steatohepatitis through AMP-activated protein kinase-independent and ULK1-mediated autophagy - Song_2023_Mol.Metab__101806
Author(s) : Song Y , Yang H , Kim J , Lee Y , Kim SH , Do IG , Park CY
Ref : Mol Metab , :101806 , 2023
Abstract : Song_2023_Mol.Metab__101806
ESTHER : Song_2023_Mol.Metab__101806
PubMedSearch : Song_2023_Mol.Metab__101806
PubMedID: 37739179

Title : Gemigliptin Alleviates Succinate-Induced Hepatic Stellate Cell Activation by Ameliorating Mitochondrial Dysfunction - Nguyen_2022_Endocrinol.Metab.(Seoul)__
Author(s) : Nguyen G , Park SY , Do DV , Choi DH , Cho EH
Ref : Endocrinol Metab (Seoul) , : , 2022
Abstract : Nguyen_2022_Endocrinol.Metab.(Seoul)__
ESTHER : Nguyen_2022_Endocrinol.Metab.(Seoul)__
PubMedSearch : Nguyen_2022_Endocrinol.Metab.(Seoul)__
PubMedID: 36377343

Title : Pharmacological profiles of gemigliptin (LC15-0444), a novel dipeptidyl peptidase-4 inhibitor, in vitro and in vivo - Kim_2016_Eur.J.Pharmacol_788_54
Author(s) : Kim SH , Jung E , Yoon MK , Kwon OH , Hwang DM , Kim DW , Kim J , Lee SM , Yim HJ
Ref : European Journal of Pharmacology , 788 :54 , 2016
Abstract : Kim_2016_Eur.J.Pharmacol_788_54
ESTHER : Kim_2016_Eur.J.Pharmacol_788_54
PubMedSearch : Kim_2016_Eur.J.Pharmacol_788_54
PubMedID: 27298192

Title : Gemigliptin, a dipeptidyl peptidase-4 inhibitor, inhibits retinal pericyte injury in db\/db mice and retinal neovascularization in mice with ischemic retinopathy - Jung_2015_Biochim.Biophys.Acta_1852_2618
Author(s) : Jung E , Kim J , Kim CS , Kim SH , Cho MH
Ref : Biochimica & Biophysica Acta , 1852 :2618 , 2015
Abstract : Jung_2015_Biochim.Biophys.Acta_1852_2618
ESTHER : Jung_2015_Biochim.Biophys.Acta_1852_2618
PubMedSearch : Jung_2015_Biochim.Biophys.Acta_1852_2618
PubMedID: 26391252

Title : Dipeptidyl petidase-IV inhibitor (gemigliptin) inhibits tunicamycin-induced endoplasmic reticulum stress, apoptosis and inflammation in H9c2 cardiomyocytes - Hwang_2014_Mol.Cell.Endocrinol_392_1
Author(s) : Hwang HJ , Jung TW , Ryu JY , Hong HC , Choi HY , Seo JA , Kim SG , Kim NH , Choi KM , Choi DS , Baik SH , Yoo HJ
Ref : Mol Cell Endocrinol , 392 :1 , 2014
Abstract : Hwang_2014_Mol.Cell.Endocrinol_392_1
ESTHER : Hwang_2014_Mol.Cell.Endocrinol_392_1
PubMedSearch : Hwang_2014_Mol.Cell.Endocrinol_392_1
PubMedID: 24813659

Title : Pharmacokinetics and pharmacodynamics of LC15-0444, a novel dipeptidyl peptidase IV inhibitor, after multiple dosing in healthy volunteers - Lim_2009_Br.J.Clin.Pharmacol_68_883
Author(s) : Lim KS , Cho JY , Kim BH , Kim JR , Kim HS , Kim DK , Kim SH , Yim HJ , Lee SH , Shin SG , Jang IJ , Yu KS
Ref : British Journal of Clinical Pharmacology , 68 :883 , 2009
Abstract : Lim_2009_Br.J.Clin.Pharmacol_68_883
ESTHER : Lim_2009_Br.J.Clin.Pharmacol_68_883
PubMedSearch : Lim_2009_Br.J.Clin.Pharmacol_68_883
PubMedID: 20002082

Title : Pharmacokinetics, pharmacodynamics, and tolerability of the dipeptidyl peptidase IV inhibitor LC15-0444 in healthy Korean men: a dose-block-randomized, double-blind, placebo-controlled, ascending single-dose, Phase I study - Lim_2008_Clin.Ther_30_1817
Author(s) : Lim KS , Kim JR , Choi YJ , Shin KH , Kim KP , Hong JH , Cho JY , Shin HS , Yu KS , Shin SG , Kwon OH , Hwang DM , Kim JA , Jang IJ
Ref : Clin Ther , 30 :1817 , 2008
Abstract : Lim_2008_Clin.Ther_30_1817
ESTHER : Lim_2008_Clin.Ther_30_1817
PubMedSearch : Lim_2008_Clin.Ther_30_1817
PubMedID: 19014837