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Aprotinin

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Chemical Structure| 9087-70-1 同义名 : 抑肽酶 ;Bovine Pancreatic Trypsin Inhibitor;BPTI;RP9921;HSDB7502
CAS号 : 9087-70-1
货号 : A328348
分子式 : -
纯度 : 3.0EPU/mg
分子量 : 0
MDL号 : MFCD00130541
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 65 mg/mL，配合低频超声，并调节pH至3，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL，配合低频超声助溶
动物实验配方：
生物活性
描述 Aprotinin is an inhibitor of serine protease which can inhibit trypsin and chymotrypsin with Ki values of 0.06 pM and 9 nM[3]. Aprotinin is also a competitive protein inhibitor of NOS activity. It inhibits NOS-I and NOS-II with Ki values of 50 μM and 78 μM, respectively[4]. Aprotinin significantly inhibits fibrinolysis with an IC50 of 0.16±0.05 μM[5]. In liver transplantation, the use of aprotinin is associated with a significant reduction in blood loss and transfusion requirements of around 30-40%[6]. Aprotinin significantly inhibited the growth of human breast cancer cell lines MDA-MB-231, SK-BR-3 and MCF-7, and normal fibroblast cell line HDF-1. Inhibition of local invasion by aprotinin was significant only in the case of MDA-MB-231[7]. Aprotinin can reduce degradation of fibrin sutures without significant effects on MSC (human mesenchymal stem cell) function[8].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00372957 Diabetes Mellitus, Type 2 Phase 2 Completed - -
NCT03423069 Irritable Bowel Syndrome Not Applicable Recruiting December 31, 2020 Italy ... 展开 >> IRCCS Saverio de Bellis Recruiting Castellana Grotte, Bari, Italy, 70013 Contact: Giuseppe Riezzo    00390804994 ext 274    giuseppe.riezzo@irccsdebellis.it 收起 <<
NCT00372957 - Completed - -
参考文献

[1]Sperzel M, Huetter J. Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost. 2007 Oct;5(10):2113-8.

[2]Fritz H, Wunderer G. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94.

[3]Fritz H, Wunderer G. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94

[4]Venturini G, Colasanti M, Ascenzi P. Aprotinin, the first competitive protein inhibitor of NOS activity. Biochem Biophys Res Commun. 1998 Aug 10;249(1):263-5

[5]Davis R, Whittington R. Aprotinin. A review of its pharmacology and therapeutic efficacy in reducing blood loss associated with cardiac surgery. Drugs. 1995 Jun;49(6):954-83

[6]Pereboom IT, de Boer MT, Porte RJ, Molenaar IQ. Aprotinin and nafamostat mesilate in liver surgery: effect on blood loss. Dig Surg. 2007;24(4):282-7

[7]Soleyman-Jahi S, Sadeghi F, Afshari Z, Barati T, Ghasemi S, Muhammadnejad S, Amanpour S, Zendehdel K. Anti-neoplastic effects of aprotinin on human breast cancer cell lines: In vitro study. Adv Clin Exp Med. 2019 Feb;28(2):151-157

[8]Coffin ST, Gaudette GR. Aprotinin extends mechanical integrity time of cell-seeded fibrin sutures. J Biomed Mater Res A. 2016 Sep;104(9):2271-9