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Aprotinin/抑肽酶 {[allProObj[0].p_purity_real_show]}

货号:A328348 同义名: 抑肽酶 / Bovine Pancreatic Trypsin Inhibitor; BPTI

Aprotinin是一种丝氨酸蛋白酶抑制剂,能抑制胰蛋白酶和胰凝乳蛋白酶,Ki 值分别为 0.06 pM 和 9 nM,用于减少术中失血和输血需求。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Aprotinin/抑肽酶 化学结构 CAS号:9087-70-1
Aprotinin/抑肽酶 化学结构
CAS号:9087-70-1
Aprotinin/抑肽酶 3D分子结构
CAS号:9087-70-1
Aprotinin/抑肽酶 化学结构 CAS号:9087-70-1
Aprotinin/抑肽酶 3D分子结构 CAS号:9087-70-1
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Aprotinin/抑肽酶 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].

Aprotinin/抑肽酶 细胞实验

Cell Line
Concentration Treated Time Description References
Human mesenchymal stem cells (MSCs) 100 μg/mL 21-28 days To assess the effect of Aprotinin on MSC multipotency, results showed MSCs could differentiate into adipocytes, osteocytes, and chondrocytes in the presence of Aprotinin. J Biomed Mater Res A. 2016 Sep;104(9):2271-9.
Human mesenchymal stem cells (MSCs) 100 μg/mL 3 days To assess the effect of Aprotinin on MSC proliferation, results showed no significant effect on cell proliferation. J Biomed Mater Res A. 2016 Sep;104(9):2271-9.
Human mesenchymal stem cells (MSCs) 100 μg/mL 7 days To assess the effect of Aprotinin on MSC viability, results showed no significant effect on cell viability. J Biomed Mater Res A. 2016 Sep;104(9):2271-9.

Aprotinin/抑肽酶 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
129S1/SvImJ mice Healthy wild-type mice Subcutaneously implanted sustained release pellets 2 mg/day or 0.5 mg/day Continuous for 10 days To investigate the impact of aprotinin treatment on sodium handling in healthy wild-type mice under control and low-salt conditions. High-dose aprotinin (2 mg/day) led to proximal tubular dysfunction, impaired sodium preservation, glucosuria, and proteinuria, and caused kidney injury. No kidney injury was observed with a lower dose (0.5 mg/day). Acta Pharmacol Sin. 2022 Jan;43(1):111-120
Fischer 344 rats Subcutaneous implant model Subcutaneous implantation 3000U/mL 7 and 14 days To evaluate the effects of aprotinin on fibrin scaffold degradation, angiogenic responses, and fibrous capsule formation. Results showed aprotinin significantly reduced scaffold degradation, increased angiogenesis, and decreased fibrous capsule thickness. Angiogenesis. 2014 Jan;17(1):195-205
BALB/c mice Influenza pneumonia model Intraperitoneal injection 50,000 KIU/kg Twice daily for 5 days Evaluated the efficacy of aprotinin in combination with antiviral drugs for influenza pneumonia, showing significant reduction in virus titer and increased survival rate. Molecules. 2022 Aug 5;27(15):4975
Dogs Canine cardiopulmonary bypass model Intravenous infusion 50,000 KIU/kg (pre-bypass), 10,000 KIU/kg/hr (post-bypass), 50,000 KIU/kg (mixed in priming solution) Pre-bypass for 20 minutes, post-bypass for 3 hours To evaluate the effect of Aprotinin on the elevation of pulmonary vascular resistance (PVR) after cardiopulmonary bypass. Results showed that PVR elevation in the aprotinin group was significantly lower than in the control group at 3 hours post-bypass (p=0.0047). Pathological examination revealed near normal lung structure in the aprotinin group compared to various inflammatory reactions in the control group. J Korean Med Sci. 2006 Feb;21(1):25-9

Aprotinin/抑肽酶 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 - -

Aprotinin/抑肽酶 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

Aprotinin/抑肽酶 技术信息

CAS号9087-70-1
SMILES Code NONE
MDL No. MFCD00130541
别名 抑肽酶 ;Bovine Pancreatic Trypsin Inhibitor; BPTI; RP9921; HSDB7502
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

溶解方案

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

配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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