アルガトロバン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

アルガトロバン 価格

アルガトロバン 化学特性,用途語,生産方法

• 外観

  白色～ほとんど白色粉末～結晶

• 効能

  抗凝固薬, トロンビン阻害薬

• 商品名

  スロンノン (第一三共); ノバスタン (田辺三菱製薬)

• 使用

  Argatroban monohydrate has been used as a thrombin-selective inhibitor in the thrombin assay of platelet poor plasma samples. It may be used as a standard in gradient reversed-phase liquid chromatography coupled with high-resolution multistage mass spectrometry (LC/HR-MSⁿ) for photoproducts fragmentation analysis and as a thrombin inhibitor competitive assay with fullerene-based C60 nanoparticle (NPs).

• 一般的な説明

  Argatroban anticoagulant is synthesized from L-arginine and photodegrades under light exposure.

• 酵素阻害剤

  This anticoagulant (FW = 508.64 g/mol; CAS 74863-84-6), also named (2R,4R) -4-methyl-1-N2-[ (3-methyl-1,2,3,4-tetrahydro-8-quinolilyl) sulfon- yl]-L-arginyl-2-piperidine carboxylic acid, Novastan?, and MD-805, is a direct thrombin inhibitor (1-11) that is an effective treatment for heparin- induced thrombocytopenia (HIT), an immunoglobulin-mediated adverse drug reaction characterized by platelet activation, thrombocytopenia, and a high risk of thrombotic complications among patients who are receiving or have recently received heparin. HIT is an autoimmune-like disorder, with the target antigen a multimolecular complex of the “self” protein, Platelet Factor-4, and heparin. Continued use of heparin is ill-advised and dangerous. Argatroban is also indicated for the treatment of heparin- induced thrombocytopenia and thrombosis syndrome (HITTS), an immune- mediated response to the administration of heparin that results in life- threatening thrombosis. Argatroban is one of four FDA-approved parenteral direct thrombin inhibitors, the others being lepirudin, desirudin, and bivalirudin. Argatroban is metabolized in the liver (t1/2 = ~50 min). Other DTI’s include recombinant hirudins, bivalirudin, and ximelagatran, either alone or in combination with melagatran. Argatroban is a significantly weaker inhibitor of trypsin, K = 4.3 μM, plasmin (K = ii 800 μM), coagulation factor Xa, and plasma kallikrein (Ki = 2 mM). Commercial sources often supply a mixture of 21 (R) and 21 (S) Diastereoisomers. The latter is more potent.

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141396-28-3, アルガトロバン キーワード