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標簽:Otamixaban
聯系人:高小姐
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化學性質:
規格 | 10mg 100mg |
CAS | 19 |
別名 | FXV 673; FXV-673; FXV673 |
化學名 | methyl (2R,3R)-2-[(3-carbamimidoylphenyl)methyl]-3-[[4-(1-oxidopyridin-1-ium-4-yl)benzoyl]amino]butanoate |
分子式 | C25H26N4O4 |
分子量 | 446.53 |
溶解度 | ≥ 22.35 mg/mL in DMSO, ≥ 55 mg/mL in EtOH with gentle warming |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
Otamixaban (FXV673) is a potent, selective, rapid acting, competitive and reversible inhibitor of factor Xa with IC50 value of 0.4 nM.[5]
Factor Xa is a serine endopeptidase which is activated into factor Xa by both factor IX with its cofactor, factor VIII known as intrinsic Xase, and factor VII with its cofactor, tissue factor. Factor Xa (fXa) is a pivotal serine protease situated at the juncture of the intrinsic and extrinsic pathways of the blood coagulation cascade.[2] Its singular role in thrombin activation and potentiating effects on clot formation makes it as a target for therapeutic intervention. FXa is responsible for the initiation of the coagulation cascade,[3] cleaving prothrombin to its active form thrombin, which then acts to convert soluble fibrinogen to insoluble fibrin and to activate platelets. Stabilization of the platelet aggregation by fibrin mesh ultimately leads to clot formation.[4] Thus, the inhibition of fXa (in the physiologically relevant prothrombinase complex) represents an attractive target for the development of novel antithrombotic agents.[5]
Otamixaban (FXV673) selectively and competitively inhibit FXa, suppressing prothrombin activity at the sites of blood clot (thrombus) formation. This leads to a decrease in blood clot formation in a dose dependent manner.[1] Reducing blood clot formation will decrease blood flow blockages, thus possibly lowering the risk of myocardial infarction, unstable angina, venous thrombosis, and ischemic stroke.[6] In conclusion, FXV673 is an effective inhibitor of fXa in the physiologically relevant human prothrombinase complex. Recently a new series of specific, direct acting inhibitors of Factor Xa has been developed. And they may be more effective against Factor Xa in that they inhibit both free Factor Xa and Factor Xa in the prothrombinase complex
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278