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Literature summary extracted from

  • Kim, K.R.; Rhee, S.D.; Kim, H.Y.; Jung, W.H.; Yang, S.D.; Kim, S.S.; Ahn, J.H.; Cheon, H.G.
    KR-62436, 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile, is a novel dipeptidyl peptidase-IV (DPP-IV) inhibitor with anti-hyperglycemic activity (2005), Eur. J. Pharmacol., 518, 63-70.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.14.5 medicine inhibition of DPP-IV can be an effective approach to treat type 2 diabetes mellitus by potentiating insulin secretion. 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile, i.e. KR-62436, could be good lead compound for further development as a new anti-diabetic agent Homo sapiens
3.4.14.5 medicine inhibition of DPP-IV can be an effective approach to treat type 2 diabetes mellitus by potentiating insulin secretion. 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile, i.e. KR-62436, could be good lead compound for further development as a new anti-diabetic agent Rattus norvegicus
3.4.14.5 medicine inhibition of DPP-IV can be an effective approach to treat type 2 diabetes mellitus by potentiating insulin secretion. 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile, i.e. KR-62436, could be good lead compound for further development as a new anti-diabetic agent Sus scrofa

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.14.5 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile i.e. KR-62436, IC50: 0.00014 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1 Homo sapiens
3.4.14.5 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile i.e. KR-62436, IC50: 0.00078 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1 Rattus norvegicus
3.4.14.5 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile i.e. KR-62436, IC50: 0.00049 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1 Sus scrofa

Organism

EC Number Organism UniProt Comment Textmining
3.4.14.5 Homo sapiens
-
-
-
3.4.14.5 Rattus norvegicus
-
-
-
3.4.14.5 Sus scrofa
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.14.5 blood plasma
-
 Rattus norvegicus
-
3.4.14.5 kidney
-
 Sus scrofa
-

Synonyms

EC Number Synonyms Comment Organism
3.4.14.5 DPP-IV
-
 Homo sapiens
3.4.14.5 DPP-IV
-
 Rattus norvegicus
3.4.14.5 DPP-IV
-
 Sus scrofa

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.14.5 0.00014
-
 i.e. KR-62436, IC50: 0.00014 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1 Homo sapiens 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
3.4.14.5 0.00049
-
 i.e. KR-62436, IC50: 0.00049 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1 Sus scrofa 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
3.4.14.5 0.00078
-
 i.e. KR-62436, IC50: 0.00078 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1 Rattus norvegicus 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile