CAS NO: | 9087-70-1 |
生物活性 | Aprotinin is abovine pancreatic trypsin inhibitor (BPTI)inhibitor which inhibitstrypsinandchymotrypsinwithKis of 0.06 pM and 9 nM, respectively. | ||||||||||||||||
IC50& Target | Ki: 0.06 pM (Trypsin), 9 nM (Chymotrypsin)[1] | ||||||||||||||||
体外研究 (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[2]. Aprotinin inhibits trypsin (bovine, Ki= 0.06 pM), chymotrypsin (bovine, Ki= 9 nM), plasmin (human, 0.23 nM)[1]. Aprotinin is also a competitive protein inhibitor of NOS activity. It inhibits NOS-I and NOS-II with Kivalues of 50 μM and 78 μM, respectively[3]. Aprotinin significantly inhibits fibrinolysis with an IC50of 0.16±0.05 μM[4]. | ||||||||||||||||
体内研究 (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[5]. Aprotinin inhibits thrombus formation in a dose-dependent manner. Aprotinin at a dose of 1.5 mg kg-1(bolus) and 3 mg kg-1h-1infusion (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-1bolus plus 6 mg kg-1h-1showing a reduction of approximately 84%±2.9%. At the highest dose of 5 mg kg-1and 10 mg kg-1h-1, the strongest effects are observed[4]. 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[6]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 6511.44 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C284H432N84O79S7 | ||||||||||||||||
CAS 号 | 9087-70-1 | ||||||||||||||||
Sequence | Arg-Pro-Asp-Phe-Cys-Leu-Glu-Pro-Pro-Tyr-Thr-Gly-Pro-Cys-Lys-Ala-Arg-Ile-Ile-Arg-Tyr-Phe-Tyr-Asn-Ala-Lys-Ala-Gly-Leu-Cys-Gln-Thr-Phe-Val-Tyr-Gly-Gly-Cys-Arg-Ala-Lys-Arg-Asn-Asn-Phe-Lys-Ser-Ala-Glu-Asp-Cys-Met-Arg-Thr-Cys-Gly-Gly-Ala(Disulfide bridge: Cys5-Cys55,Cys14-Cys38,Cys30-Cys51) | ||||||||||||||||
Sequence Shortening | RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA(Disulfide bridge: Cys5-Cys55,Cys14-Cys38,Cys30-Cys51) | ||||||||||||||||
中文名称 | 抑肽酶;抑胰肽酶;屈来密多 | ||||||||||||||||
结构分类 |
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来源 | Bovine lung | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | Sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: H2O : 100 mg/mL(15.36 mM;Need ultrasonic) DMSO : 66.67 mg/mL(10.24 mM;ultrasonic and adjust pH to 3 with HCl) 配制储备液
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以下溶剂前显示的百
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