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Literature summary extracted from

  • Chu, V.; Brown, K.; Colussi, D.; Gao, J.; Bostwick, J.; Kasiewski, C.; Bentley, R.; Morgan, S.; Guertin, K.; Pauls, H.W.; Gong, Y.; Zulli, A.; Perrone, M.H.; Dunwiddie, C.T.; Leadley, R.J.
    Pharmacological characterization of a novel factor Xa inhibitor, FXV673 (2001), Thromb. Res., 103, 309-324.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.6 2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester i.e. FXV673, highly specific fo factor Xa compared to other serine protesases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, inhibition of thrombus formation in vivo in the acute arterial and venous electrolytic injury canine model, no effect on platelet aggregation Canis lupus familiaris
3.4.21.6 2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester i.e. FXV673, highly specific fo factor Xa compared to other serine proteases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, no effect on platelet aggregation Homo sapiens
3.4.21.6 2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester i.e. FXV673, highly specific fo factor Xa compared to other serine protesases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, no effect on platelet aggregation Oryctolagus cuniculus
3.4.21.6 EDTA
-
 Canis lupus familiaris
3.4.21.6 EDTA
-
 Homo sapiens
3.4.21.6 EDTA
-
 Oryctolagus cuniculus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.21.6 extracellular
-
 Homo sapiens
-
-
3.4.21.6 extracellular
-
 Oryctolagus cuniculus
-
-
3.4.21.6 extracellular
-
 Canis lupus familiaris
-
-

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.6 Canis lupus familiaris
-
 mongrel dogs of either sex
-
3.4.21.6 Homo sapiens
-
-
-
3.4.21.6 Oryctolagus cuniculus
-
-
-

Reaction

EC Number Reaction Comment Organism Reaction ID
3.4.21.6 selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Homo sapiens
a
3.4.21.6 selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Oryctolagus cuniculus
a
3.4.21.6 selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Canis lupus familiaris
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.6 commercial preparation
-
 Homo sapiens
-
3.4.21.6 commercial preparation
-
 Oryctolagus cuniculus
-
3.4.21.6 commercial preparation
-
 Canis lupus familiaris
-
3.4.21.6 plasma
-
 Homo sapiens
-
3.4.21.6 plasma
-
 Oryctolagus cuniculus
-
3.4.21.6 plasma
-
 Canis lupus familiaris
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.6 prothrombin + H2O
-
 Homo sapiens thrombin + ?
-
 ?
3.4.21.6 prothrombin + H2O
-
 Oryctolagus cuniculus thrombin + ?
-
 ?
3.4.21.6 prothrombin + H2O
-
 Canis lupus familiaris thrombin + ?
-
 ?

Subunits

EC Number Subunits Comment Organism
3.4.21.6 More enzyme is part of the prothrombinase enzyme complex including also factor Va, phospholipids and Ca2+ Homo sapiens
3.4.21.6 More enzyme is part of the prothrombinase enzyme complex including also factor Va, phospholipids and Ca2+ Oryctolagus cuniculus
3.4.21.6 More enzyme is part of the prothrombinase enzyme complex including also factor Va, phospholipids and Ca2+ Canis lupus familiaris

Synonyms

EC Number Synonyms Comment Organism
3.4.21.6 factor Xa
-
 Homo sapiens
3.4.21.6 factor Xa
-
 Oryctolagus cuniculus
3.4.21.6 factor Xa
-
 Canis lupus familiaris
3.4.21.6 FXa
-
 Homo sapiens
3.4.21.6 FXa
-
 Oryctolagus cuniculus
3.4.21.6 FXa
-
 Canis lupus familiaris
3.4.21.6 More the enzyme belongs to the peptidase family S1, i.e. trypsin family Homo sapiens
3.4.21.6 More the enzyme belongs to the peptidase family S1, i.e. trypsin family Oryctolagus cuniculus
3.4.21.6 More the enzyme belongs to the peptidase family S1, i.e. trypsin family Canis lupus familiaris

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.21.6 37
-
 assay at Canis lupus familiaris

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.21.6 7.5
-
 assay at Homo sapiens
3.4.21.6 7.5
-
 assay at Oryctolagus cuniculus
3.4.21.6 7.5
-
 assay at Canis lupus familiaris

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.6 0.00000027
-
 2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester pH 7.5, 37°C Oryctolagus cuniculus
3.4.21.6 0.00000052
-
 2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester pH 7.5, 37°C Homo sapiens
3.4.21.6 0.00000141
-
 2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester pH 7.5, 37°C Canis lupus familiaris