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Literature summary for 3.4.21.6 extracted from

  • Hayashi, M.; Matsuo, A.; Nakamoto, H.; Aisaka, K.
    Antithrombotic effects of a synthetic inhibitor of activated factor X, JTV-803, in animals (2001), Eur. J. Pharmacol., 412, 61-66.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate i.e. JTV-803, strong, synthetic inhibitor highly specific for factor Xa compared to other serine proteases Homo sapiens
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate i.e. JTV-803, synthetic the enzyme in vitro and thrombus formation in rats in vivo Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
prothrombin + H2O Homo sapiens
-
thrombin + ?
-
?
prothrombin + H2O Rattus norvegicus
-
thrombin + ?
-
?

Organism

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

Reaction

Reaction Comment Organism Reaction ID
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Homo sapiens
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
artery middle cerebral Rattus norvegicus
-
blood
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
prothrombin + H2O
-
Homo sapiens thrombin + ?
-
?
prothrombin + H2O
-
Rattus norvegicus thrombin + ?
-
?

Synonyms

Synonyms Comment Organism
More the enzyme belongs to the peptidase family S1, i.e. trypsin family Homo sapiens
More the enzyme belongs to the peptidase family S1, i.e. trypsin family Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000019
-
4-{[(2-carbamimidoyl-1,2,3,4-tetrahydroisoquinolin-7-yl)oxy]methyl}-1-(pyridin-4-yl)piperidine-4-carboxylic acid methanesulfonate
-
Homo sapiens