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Literature summary for 3.4.14.5 extracted from

  • Someya, Y.; Tahara, A.; Nakano, R.; Matsuyama-Yokono, A.; Nagase, I.; Fukunaga, Y.; Takasu, T.; Hayakawa, M.; Shibasaki, M.
    Pharmacological profile of ASP8497, a novel, selective, and competitive dipeptidyl peptidase-IV inhibitor, in vitro and in vivo (2008), Naunyn Schmiedebergs Arch. Pharmacol., 377, 209-217.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
ASP8497 potent, selective, and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity, i.e. (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate Canis lupus familiaris
ASP8497 potent, selective, and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity, i.e. (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate Homo sapiens
ASP8497 potent, selective, and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity, i.e. (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate Mus musculus
vildagliptin LAF237, 1-[[3-hydroxy-1-adamantyl]amino]acetyl-2-cyano-(S)-pyrrolidine Canis lupus familiaris
vildagliptin LAF237, 1-[[3-hydroxy-1-adamantyl]amino]acetyl-2-cyano-(S)-pyrrolidine Homo sapiens
vildagliptin LAF237, 1-[[3-hydroxy-1-adamantyl]amino]acetyl-2-cyano-(S)-pyrrolidine Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
glucagon-like peptide 1 + H2O Mus musculus
-
?
-
?
glucagon-like peptide 1 + H2O Homo sapiens
-
?
-
?
glucagon-like peptide 1 + H2O Canis lupus familiaris
-
?
-
?

Organism

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

Source Tissue

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glucagon-like peptide 1 + H2O
-
Mus musculus ?
-
?
glucagon-like peptide 1 + H2O
-
Homo sapiens ?
-
?
glucagon-like peptide 1 + H2O
-
Canis lupus familiaris ?
-
?
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
-
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
-
Canis lupus familiaris
DPP-IV
-
Mus musculus
DPP-IV
-
Homo sapiens
DPP-IV
-
Canis lupus familiaris

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000052
-
ASP8497 median inhibition concentration, in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% bovine serum albumin, at pH 7.3 and 25°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000026
-
median inhibition concentration, in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% bovine serum albumin, at pH 7.3 and 25°C Mus musculus ASP8497
0.0000062
-
median inhibition concentration, in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% bovine serum albumin, at pH 7.3 and 25°C Homo sapiens ASP8497
0.0000073
-
median inhibition concentration, in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% bovine serum albumin, at pH 7.3 and 25°C Canis lupus familiaris ASP8497