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Literature summary for 3.4.14.5 extracted from

  • Matsuyama-Yokono, A.; Tahara, A.; Nakano, R.; Someya, Y.; Nagase, I.; Hayakawa, M.; Shibasaki, M.
    ASP8497 is a novel selective and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity (2008), Biochem. Pharmacol., 76, 98-107.
    View publication on PubMed
Search for more literature for 3.4.14.5

Inhibitors

Inhibitors Comment Organism Structure
ASP-8497 (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, selective and competitive inhibitor of DPP-IV, ASP8497 is a DPP-IV inhibitor with long-acting antidiabetic effect that might be a potential agent for type 2 diabetes Canis lupus familiaris
ASP-8497 (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, selective and competitive inhibitor of DPP-IV, ASP8497 is a DPP-IV inhibitor with long-acting antidiabetic effect that might be a potential agent for type 2 diabetes Homo sapiens
ASP-8497 (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, selective and competitive inhibitor of DPP-IV, ASP8497 is a DPP-IV inhibitor with long-acting antidiabetic effect that might be a potential agent for type 2 diabetes Mus musculus
ASP-8497 (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, selective and competitive inhibitor of DPP-IV, ASP8497 is a DPP-IV inhibitor with long-acting antidiabetic effect that might be a potential agent for type 2 diabetes Rattus norvegicus
saxagliptin
-
 Canis lupus familiaris
saxagliptin
-
 Homo sapiens
saxagliptin
-
 Mus musculus
saxagliptin
-
 Rattus norvegicus
sitagliptin
-
 Canis lupus familiaris
sitagliptin
-
 Homo sapiens
sitagliptin
-
 Mus musculus
sitagliptin
-
 Rattus norvegicus
vildagliptin
-
 Canis lupus familiaris
vildagliptin
-
 Homo sapiens
vildagliptin
-
 Mus musculus
vildagliptin
-
 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Canis lupus familiaris
-
-
-
Homo sapiens
-
-
-
Mus musculus
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
 Mus musculus
-
blood plasma
-
 Homo sapiens
-
blood plasma
-
 Rattus norvegicus
-
blood plasma
-
 Canis lupus familiaris
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Gly-L-Pro-7-amido-4-methylcoumarin + H2O
-
 Mus musculus Gly-L-Pro + 7-amino-4-methylcoumarin
-
 ?
Gly-L-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Gly-L-Pro + 7-amino-4-methylcoumarin
-
 ?
Gly-L-Pro-7-amido-4-methylcoumarin + H2O
-
 Rattus norvegicus Gly-L-Pro + 7-amino-4-methylcoumarin
-
 ?
Gly-L-Pro-7-amido-4-methylcoumarin + H2O
-
 Canis lupus familiaris Gly-L-Pro + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase-IV
-
 Mus musculus
dipeptidyl peptidase-IV
-
 Homo sapiens
dipeptidyl peptidase-IV
-
 Rattus norvegicus
dipeptidyl peptidase-IV
-
 Canis lupus familiaris
DPP-IV
-
 Mus musculus
DPP-IV
-
 Homo sapiens
DPP-IV
-
 Rattus norvegicus
DPP-IV
-
 Canis lupus familiaris

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000167
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Rattus norvegicus vildagliptin
0.00000171
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Rattus norvegicus saxagliptin
0.00000236
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Rattus norvegicus ASP-8497
0.00000257
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Mus musculus saxagliptin
0.00000324
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Mus musculus vildagliptin
0.00000337
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Homo sapiens saxagliptin
0.00000347
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Canis lupus familiaris vildagliptin
0.00000386
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Mus musculus ASP-8497
0.00000422
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Canis lupus familiaris saxagliptin
0.00000528
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Homo sapiens vildagliptin
0.0000053
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Homo sapiens ASP-8497
0.00000553
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Canis lupus familiaris ASP-8497
0.00000996
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Homo sapiens sitagliptin
0.0000108
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Canis lupus familiaris sitagliptin
0.0000115
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Rattus norvegicus sitagliptin
0.0000213
-
 in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C Mus musculus sitagliptin