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Inhibitor Report for: Cofrogliptin

Inhibition of human recombinant DPP4 incubated for 15 mins using Gly-Pro-7-AMC substrate IC50 0.0042 microM


General
Type Gliptin, Trifluo, 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
IUPHAR|
Wikipedia|

Target
Families | Cofrogliptin ligand of proteins in family: DPP4N_Peptidase_S9
Protein | human-DPP4

References:
Search PubMed for references concerning: Cofrogliptin
    Title: Pharmacokinetics, Pharmacodynamics, and Safety of Single Dose HSK7653 Tablets in Chinese Subjects with Normal or Impaired Renal Function
    Shi D, Chen L, Li G, Wu N, Zhang F, Wang X, Mu N, Chen X, Yang X and Zhang D <3 more author(s)>
    Ref: Clinical Pharmacokinetics, :, 2024 : PubMed

            

    Title: A model-informed approach to accelerate the clinical development of cofrogliptin (HSK7653), a novel ultralong-acting dipeptidyl peptidase-4 inhibitor
    Cui C, Cao F, Kong, II, Wu Q, Li F, Li H, Liu D
    Ref: Diabetes Obes Metab, :, 2023 : PubMed

            

    Title: Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes
    Zhang C, Ye F, Wang J, He P, Lei M, Huang L, Huang A, Tang P, Lin H and Yan P <3 more author(s)>
    Ref: Journal of Medicinal Chemistry, 63:7108, 2020 : PubMed