Cofrogliptin
Inhibition of human recombinant DPP4 incubated for 15 mins using Gly-Pro-7-AMC substrate IC50 0.0042 microM
General
Type : Gliptin, Trifluoro, Pyrazole, Sulfonamide, Sulfur Compound
Chemical_Nomenclature : 1(2R,3S,5R,6S)-2-(2,5-difluorophenyl)-5-(2-methylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)-6-(trifluoromethyl)oxan-3-amine
Canonical SMILES : CS(=O)(=O)N1C=C2CN(CC2=N1)C3CC(C(OC3C(F)(F)F)C4=C(C=CC(=C4)F)F)N
InChI : InChI=1S\/C18H19F5N4O3S\/c1-31(28,29)27-7-9-6-26(8-14(9)25-27)15-5-13(24)16(30-17(15)18(21,22)23)11-4-10(19)2-3-12(11)20\/h2-4,7,13,15-17H,5-6,8,24H2,1H3\/t13-,15+,16+,17-\/m0\/s1
InChIKey : GUBOXFWNNXSQNH-SVGFKBNWSA-N
Other name(s) : HSK7653 || Haisco HSK 7653 || LH4G6K6NKP || CHEMBL4646510
MW : 466.4
Formula : C18H19F5N4O3S
CAS_number :
PubChem : 118613788
UniChem : GUBOXFWNNXSQNH-SVGFKBNWSA-N
Target
Families : Cofrogliptin ligand of proteins in family
DPP4N_Peptidase_S9
Protein :
human-DPP4
References (4)
| Title : Pharmacokinetics, Pharmacodynamics, and Safety of Single Dose HSK7653 Tablets in Chinese Subjects with Normal or Impaired Renal Function - Shi_2024_Clin.Pharmacokinet__ |
| Author(s) : Shi D , Chen L , Li G , Wu N , Zhang F , Wang X , Mu N , Chen X , Yang X , Lu J , Lu Y , Wang M , Zhang D |
| Ref : Clinical Pharmacokinetics , : , 2024 |
| Abstract : |
| PubMedSearch : Shi_2024_Clin.Pharmacokinet__ |
| PubMedID: 38184489 |
| Title : Concentration-QTc Modeling of the DPP-4 Inhibitor HSK7653 in a First-in-Human Study of Chinese Healthy Volunteers - Wang_2024_Clin.Pharmacol.Drug.Dev__ |
| Author(s) : Wang X , Liu H , Cui C , Niu X , Li H , Niu S , Yan P , Wu N , Li F , Wu Q , Chen K , Hu B , Liu D |
| Ref : Clin Pharmacol Drug Dev , : , 2024 |
| Abstract : |
| PubMedSearch : Wang_2024_Clin.Pharmacol.Drug.Dev__ |
| PubMedID: 38757550 |
| Title : A model-informed approach to accelerate the clinical development of cofrogliptin (HSK7653), a novel ultralong-acting dipeptidyl peptidase-4 inhibitor - Cui_2023_Diabetes.Obes.Metab__ |
| Author(s) : Cui C , Cao F , Kong, II , Wu Q , Li F , Li H , Liu D |
| Ref : Diabetes Obes Metab , : , 2023 |
| Abstract : |
| PubMedSearch : Cui_2023_Diabetes.Obes.Metab__ |
| PubMedID: 37953687 |
| Title : Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes - Zhang_2020_J.Med.Chem_63_7108 |
| Author(s) : Zhang C , Ye F , Wang J , He P , Lei M , Huang L , Huang A , Tang P , Lin H , Liao Y , Liang Y , Ni J , Yan P |
| Ref : Journal of Medicinal Chemistry , 63 :7108 , 2020 |
| Abstract : |
| PubMedSearch : Zhang_2020_J.Med.Chem_63_7108 |
| PubMedID: 32452679 |