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Literature summary for 3.4.14.5 extracted from

  • Thomas, L.; Eckhardt, M.; Langkopf, E.; Tadayyon, M.; Himmelsbach, F.; Mark, M.
    (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with oth (2008), J. Pharmacol. Exp. Ther., 325, 175-182.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
alogliptin
-
Homo sapiens
alogliptin
-
Mus musculus
alogliptin
-
Rattus norvegicus
BI 1356 competitive inhibitor, i.e. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione, proposed trade name Ondero, BI 1356 is more than 10000fold selective for DPP-4 than DPP-8, DPP-9, aminopeptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin and is 90-fold more selective than for fibroblast activation protein in vitro Homo sapiens
BI 1356 competitive inhibitor, i.e. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione, proposed trade name Ondero, BI 1356 is more than 10000fold selective for DPP-4 than DPP-8, DPP-9, aminopeptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin and is 90-fold more selective than for fibroblast activation protein in vitro Mus musculus
BI 1356 competitive inhibitor, i.e. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione, proposed trade name Ondero, BI 1356 is more than 10000fold selective for DPP-4 than DPP-8, DPP-9, aminopeptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin and is 90-fold more selective than for fibroblast activation protein in vitro Rattus norvegicus
saxagliptin
-
Homo sapiens
saxagliptin
-
Mus musculus
saxagliptin
-
Rattus norvegicus
sitagliptin
-
Homo sapiens
sitagliptin
-
Mus musculus
sitagliptin
-
Rattus norvegicus
vildagliptin
-
Homo sapiens
vildagliptin
-
Mus musculus
vildagliptin
-
Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
glucagon-like peptide + H2O Mus musculus
-
?
-
?
glucagon-like peptide + H2O Homo sapiens
-
?
-
?
glucagon-like peptide + H2O Rattus norvegicus
-
?
-
?
glucose-dependent insulinotropic peptide + H2O Mus musculus
-
?
-
?
glucose-dependent insulinotropic peptide + H2O Homo sapiens
-
?
-
?
glucose-dependent insulinotropic peptide + H2O Rattus norvegicus
-
?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Mus musculus
-
blood plasma
-
Rattus norvegicus
-
Caco-2 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glucagon-like peptide + H2O
-
Mus musculus ?
-
?
glucagon-like peptide + H2O
-
Homo sapiens ?
-
?
glucagon-like peptide + H2O
-
Rattus norvegicus ?
-
?
glucose-dependent insulinotropic peptide + H2O
-
Mus musculus ?
-
?
glucose-dependent insulinotropic peptide + H2O
-
Homo sapiens ?
-
?
glucose-dependent insulinotropic peptide + H2O
-
Rattus norvegicus ?
-
?
H-Ala-L-Pro-7-amido-4-methylcoumarin + H2O
-
Mus musculus H-Ala-L-Pro + 7-amino-4-methylcoumarin
-
?
H-Ala-L-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens H-Ala-L-Pro + 7-amino-4-methylcoumarin
-
?
H-Ala-L-Pro-7-amido-4-methylcoumarin + H2O
-
Rattus norvegicus H-Ala-L-Pro + 7-amino-4-methylcoumarin
-
?

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase 4
-
Mus musculus
dipeptidyl peptidase 4
-
Homo sapiens
dipeptidyl peptidase 4
-
Rattus norvegicus
DPP-4
-
Mus musculus
DPP-4
-
Homo sapiens
DPP-4
-
Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
BI 1356
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000001
-
in 100 mM Tris-HCl, 100 mM NaCl, pH 7.8 Homo sapiens BI 1356
0.000019
-
in 100 mM Tris-HCl, 100 mM NaCl, pH 7.8 Homo sapiens sitagliptin
0.000024
-
in 100 mM Tris-HCl, 100 mM NaCl, pH 7.8 Homo sapiens alogliptin
0.00005
-
in 100 mM Tris-HCl, 100 mM NaCl, pH 7.8 Homo sapiens saxagliptin
0.000062
-
in 100 mM Tris-HCl, 100 mM NaCl, pH 7.8 Homo sapiens vildagliptin