Cloned (Comment) | Organism |
---|---|
expressed using baculovirus | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
alogliptin | nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase, about 75% inhibition of DPP-4 24 h after treatment with 3 mg/kg alogliptin | Canis lupus familiaris | |
alogliptin | nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase | Homo sapiens | |
alogliptin | nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase, about 15% inhibition of DPP-4 24 h after treatment with 3 mg/kg alogliptin | Macaca fascicularis | |
alogliptin | nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase, complete inhibition of DPP-4 24 h after treatment with 10 mg/kg alogliptin | Rattus norvegicus | |
sitagliptin | (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine | Canis lupus familiaris | |
sitagliptin | (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine | Homo sapiens | |
sitagliptin | (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine | Macaca fascicularis | |
sitagliptin | (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine | Rattus norvegicus | |
vildagliptin | i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine | Canis lupus familiaris | |
vildagliptin | i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine | Homo sapiens | |
vildagliptin | i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine | Macaca fascicularis | |
vildagliptin | i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine | Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Canis lupus familiaris | - |
- |
- |
Homo sapiens | - |
- |
- |
Macaca fascicularis | - |
- |
- |
Rattus norvegicus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
blood plasma | - |
Homo sapiens | - |
blood plasma | - |
Rattus norvegicus | - |
blood plasma | - |
Canis lupus familiaris | - |
blood plasma | - |
Macaca fascicularis | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O | - |
Homo sapiens | L-Ala-L-Pro + 7-amino-4-methylcoumarin | - |
? | |
L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O | - |
Rattus norvegicus | L-Ala-L-Pro + 7-amino-4-methylcoumarin | - |
? | |
L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O | - |
Canis lupus familiaris | L-Ala-L-Pro + 7-amino-4-methylcoumarin | - |
? | |
L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O | - |
Macaca fascicularis | L-Ala-L-Pro + 7-amino-4-methylcoumarin | - |
? |
Synonyms | Comment | Organism |
---|---|---|
dipeptidyl peptidase-4 | - |
Homo sapiens |
dipeptidyl peptidase-4 | - |
Rattus norvegicus |
dipeptidyl peptidase-4 | - |
Canis lupus familiaris |
dipeptidyl peptidase-4 | - |
Macaca fascicularis |
DPP-4 | - |
Homo sapiens |
DPP-4 | - |
Rattus norvegicus |
DPP-4 | - |
Canis lupus familiaris |
DPP-4 | - |
Macaca fascicularis |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000069 | - |
- |
Homo sapiens | alogliptin | |
0.0000121 | - |
- |
Homo sapiens | sitagliptin | |
0.0000238 | - |
- |
Homo sapiens | vildagliptin |