Trelagliptin

Almost identical to Alogliptin which is a selective, orally bioavailable, pyrimidinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Trelagliptin is a fluride derivative.

General

Type : Drug,Piperidine,Pyrimidine,Cyanide,Gliptin

Chemical_Nomenclature : 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]-4-fluorobenzonitrile

Canonical SMILES : CN1C(=O)C=C(N(C1=O)CC2=C(C=CC(=C2)F)C#N)N3CCCC(C3)N

InChI : InChI=1S\/C18H20FN5O2\/c1-22-17(25)8-16(23-6-2-3-15(21)11-23)24(18(22)26)10-13-7-14(19)5-4-12(13)9-20\/h4-5,7-8,15H,2-3,6,10-11,21H2,1H3\/t15-\/m1\/s1

InChIKey : IWYJYHUNXVAVAA-OAHLLOKOSA-N

Other name(s) : SYR-472,SYR-472, Zafatek,Trelagliptin(SYR-472),UNII-Q836OWG55H,Trelagliptin [USAN]


MW : 357.38

Formula : C18H20FN5O2

CAS_number : 865759-25-7

PubChem : 15983988

UniChem : IWYJYHUNXVAVAA-OAHLLOKOSA-N

IUPHAR :

Wikipedia :

Target

Families : Trelagliptin ligand of proteins in family: DPP4N_Peptidase_S9

Stucture : 5KBY Crystal structure of dipeptidyl peptidase IV in complex with SYR-472

Protein : human-DPP4

References (7)

Title : Trelagliptin ameliorates IL-1beta-impaired chondrocyte function via the AMPK\/SOX-9 pathway - Liu_2021_Mol.Immunol_140_70
Author(s) : Liu J , Zuo Q , Li Z , Chen J , Liu F
Ref : Mol Immunol , 140 :70 , 2021
Abstract : Liu_2021_Mol.Immunol_140_70
ESTHER : Liu_2021_Mol.Immunol_140_70
PubMedSearch : Liu_2021_Mol.Immunol_140_70
PubMedID: 34666245

Title : Safety evaluation of trelagliptin in the treatment of Japanese type 2 diabetes mellitus patients - Kaku_2017_Expert.Opin.Drug.Saf_16_1313
Author(s) : Kaku K
Ref : Expert Opin Drug Safety , 16 :1313 , 2017
Abstract : Kaku_2017_Expert.Opin.Drug.Saf_16_1313
ESTHER : Kaku_2017_Expert.Opin.Drug.Saf_16_1313
PubMedSearch : Kaku_2017_Expert.Opin.Drug.Saf_16_1313
PubMedID: 28829213

Title : Trelagliptin (SYR-472, Zafatek), Novel Once-Weekly Treatment for Type 2 Diabetes, Inhibits Dipeptidyl Peptidase-4 (DPP-4) via a Non-Covalent Mechanism - Grimshaw_2016_PLoS.One_11_e0157509
Author(s) : Grimshaw CE , Jennings A , Kamran R , Ueno H , Nishigaki N , Kosaka T , Tani A , Sano H , Kinugawa Y , Koumura E , Shi L , Takeuchi K
Ref : PLoS ONE , 11 :e0157509 , 2016
Abstract : Grimshaw_2016_PLoS.One_11_e0157509
ESTHER : Grimshaw_2016_PLoS.One_11_e0157509
PubMedSearch : Grimshaw_2016_PLoS.One_11_e0157509
PubMedID: 27328054
Gene_locus related to this paper: human-DPP4

Title : Effect of trelagliptin on vascular endothelial functions and serum adiponectin level in patients with type 2 diabetes: a preliminary single-arm prospective pilot study - Ida_2016_Cardiovasc.Diabetol_15_153
Author(s) : Ida S , Murata K , Betou K , Kobayashi C , Ishihara Y , Imataka K , Uchida A , Monguchi K , Kaneko R , Fujiwara R , Takahashi H
Ref : Cardiovasc Diabetol , 15 :153 , 2016
Abstract : Ida_2016_Cardiovasc.Diabetol_15_153
ESTHER : Ida_2016_Cardiovasc.Diabetol_15_153
PubMedSearch : Ida_2016_Cardiovasc.Diabetol_15_153
PubMedID: 27809903

Title : First novel once-weekly DPP-4 inhibitor, trelagliptin, for the treatment of type 2 diabetes mellitus - Kaku_2015_Expert.Opin.Pharmacother_16_2539
Author(s) : Kaku K
Ref : Expert Opin Pharmacother , 16 :2539 , 2015
Abstract : Kaku_2015_Expert.Opin.Pharmacother_16_2539
ESTHER : Kaku_2015_Expert.Opin.Pharmacother_16_2539
PubMedSearch : Kaku_2015_Expert.Opin.Pharmacother_16_2539
PubMedID: 26523434

Title : Trelagliptin: First Global Approval - McKeage_2015_Drugs_75_1161
Author(s) : McKeage K
Ref : Drugs , 75 :1161 , 2015
Abstract : McKeage_2015_Drugs_75_1161
ESTHER : McKeage_2015_Drugs_75_1161
PubMedSearch : McKeage_2015_Drugs_75_1161
PubMedID: 26115728

Title : SYR-472, a novel once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor, in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial - Inagaki_2014_Lancet.Diabetes.Endocrinol_2_125
Author(s) : Inagaki N , Onouchi H , Sano H , Funao N , Kuroda S , Kaku K
Ref : Lancet Diabetes Endocrinol , 2 :125 , 2014
Abstract : Inagaki_2014_Lancet.Diabetes.Endocrinol_2_125
ESTHER : Inagaki_2014_Lancet.Diabetes.Endocrinol_2_125
PubMedSearch : Inagaki_2014_Lancet.Diabetes.Endocrinol_2_125
PubMedID: 24622716