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Literature summary extracted from

  • Heran, C.; Morgan, S.; Kasiewski, C.; Bostwick, J.; Bentley, R.; Klein, S.; Chu, V.; Brown, K.; Colussi, D.; Czekaj, M.; Perrone, M.; Leadley, R.
    Antithrombotic efficacy of RPR208566, a novel factor Xa inhibitor, in a rat model of carotid artery thrombosis (2000), Eur. J. Pharmacol., 389, 201-207.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.21.6 pharmacology the enzyme is a target for development of antithrombotic drug therapy mechanism Homo sapiens
3.4.21.6 pharmacology the enzyme is a target for development of antithrombotic drug therapy mechanism Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.6 methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate i.e. RPR208566, highly specific Homo sapiens
3.4.21.6 methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate i.e. RPR208566, inhibits thrombus formation in the rat artery model, highly specific Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.21.6 extracellular
-
 Homo sapiens
-
-
3.4.21.6 extracellular
-
 Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.21.6 prothrombin + H2O Homo sapiens initial step in thrombus formation thrombin + ?
-
 ?
3.4.21.6 prothrombin + H2O Rattus norvegicus initial step in thrombus formation thrombin + ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.6 Homo sapiens
-
-
-
3.4.21.6 Rattus norvegicus
-
 male Spreague-Dawley
-

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 Rattus norvegicus
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.6 blood
-
 Rattus norvegicus
-
3.4.21.6 carotid artery
-
 Rattus norvegicus
-
3.4.21.6 commercial preparation
-
 Homo sapiens
-
3.4.21.6 plasma
-
 Homo sapiens
-
3.4.21.6 plasma
-
 Rattus norvegicus
-

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
-
 Rattus norvegicus thrombin + ?
-
 ?
3.4.21.6 prothrombin + H2O initial step in thrombus formation Homo sapiens thrombin + ?
-
 ?
3.4.21.6 prothrombin + H2O initial step in thrombus formation Rattus norvegicus thrombin + ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.6 coagulation factor Xa
-
 Homo sapiens
3.4.21.6 coagulation factor Xa
-
 Rattus norvegicus
3.4.21.6 factor Xa
-
 Homo sapiens
3.4.21.6 factor Xa
-
 Rattus norvegicus
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 Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.21.6 37
-
 assay at Homo sapiens
3.4.21.6 37
-
 assay at Rattus norvegicus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.6 0.0000013
-
 methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate 37°C Homo sapiens