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Aprotinin

CAS No. : 9087-70-1

MCE 站：Aprotinin

产品活性：Aprotinin是分离自牛肺的丝氨酸蛋白酶 (BPTI) 抑制剂，对胰蛋白酶和胰凝乳蛋白酶胰凝乳蛋白酶的 K_i 值分别为0.06 pM和9 nM。

研究领域：Anti-infection

作用靶点：Influenza Virus

In Vitro: Aprotinin, a serine protease inhibitor isolated from bovine lung, is a complex protease inhibitor that is an antifibrinolytic, inhibits contact activation, and decreases the inflammatory response to cardiopulmonary bypass. Aprotinin inhibits trypsin (bovine, K_i= 0.06 pM), chymotrypsin (bovine, K_i= 9 nM), plasmin (human, 0.23 nM). Aprotinin is also a competitive protein inhibitor of NOS activity. It inhibits NOS-I and NOS-II with K_i values of 50 μM and 78 μM, respectively. Aprotinin significantly inhibits fibrinolysis with an IC₅₀ of 0.16±0.05 μM.

In Vivo: High dose aprotinin can reduce blood loss and transfusion requirements associated with primary cardiac procedures such as coronary artery bypass graft (CABG) or heart valve replacement surgery. Aprotinin inhibits thrombus formation in a dose-dependent manner. Aprotinin at a dose of 1.5 mg kg^-1 (bolus) and 3 mg kg^-1 h^-1 infusion (maintenance infusion) causes a tendency towards a reduction in bleeding time. Aprotinin significantly reduces the bleeding time starting at a dose of 3 mg kg^-1 bolus plus 6 mg kg^-1 h^-1 showing a reduction of approximately 84%±2.9%. At the highest dose of 5 mg kg^-1 and 10 mg kg^-1 h^-1, the strongest effects are observed. Aprotinin may affect tumor necrosis factor-alpha (TNF) levels. Soluble TNFRI levels are significantly increased following I/R in the aprotinin treated wild type mice and not detected in all TNFRInull mice.

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