Aprotinin
Aprotinin(CAS 9087-70-1), also referred to as bovine pancreatic trypsin inhibitor (BPTI), is a naturally derived serine protease inhibitor that functions primarily through reversible inhibition of serine proteases, including trypsin, plasmin, and kallikrein. This inhibition results in decreased fibrinolysis, contributing to reduced perioperative blood loss. Consequently, aprotinin is routinely employed in surgical research, particularly in cardiovascular surgery settings, to study its role in controlling excessive bleeding and minimizing transfusion requirements during operations involving elevated fibrinolytic activity. Reported inhibitory constants (IC50) values for aprotinin typically range between 0.06 - 0.80 µM depending on targeted proteases and assay conditions.
Reference:
1. Henry DA, Carless PA, Moxey AJ, et al. Anti-fibrinolytic use for minimising perioperative allogeneic blood transfusion. Cochrane Database Syst Rev 2007; 4: CD001886.
2. Levi M, Cromheecke ME, de Jonge E, et al. Pharmacological strategies to decrease excessive blood loss in cardiac surgery: a meta-analysis of clinically relevant endpoints. Lancet 1999; 354: 1940-7.
3. Sedrakyan A, Treasure T, Elefteriades JA. Effect of aprotinin on clinical outcomes in coronary artery bypass graft surgery: a systematic review and meta-analysis of randomized clinical trials. J Thorac Cardiovasc Surg 2004; 128: 442-8.
4. Brown JR, Birkmeyer NJ, O’Connor GT. Meta-analysis comparing the effectiveness and adverse outcomes of antifibrinolytic agents in cardiac surgery. Circulation 2007; 115: 2801-13.
5. Dean A. Fergusson, Paul C. Hébert et al, A Comparison of Aprotinin and Lysine Analogues in High-Risk Cardiac Surgery, N Engl J Med 2008; 358: 2319-2331
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- 2. Yan Chen, Jiafu Zhu, et al. "Protocol for affordable and efficient profiling of nascent RNAs in bread wheat using GRO-seq." STAR Protoc. 2022 Sep 16;3(3):101657. PMID: 36097381
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- 5. Sebastian Himbert, Syed M Qadri, et al. "Blood bank storage of red blood cells increases RBC cytoplasmic membrane order and bending rigidity." PLoS One. 2021 Nov 12;16(11):e0259267. PMID: 34767588
- 6. Angelo D'Alessandro, Tiffany Thomas, et al. "Biological and Clinical Factors Contributing to the Metabolic Heterogeneity of Hospitalized Patients with and without COVID-19." Cells. 2021 Sep 2;10(9):2293. PMID: 34571942
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 6511.44 |
| Cas No. | 9087-70-1 |
| Formula | C284H432N84O79S7 |
| Synonyms | Aprotinin, Trypsin inhibitor (basic) |
| Solubility | ≥195 mg/mL in H2O; insoluble in DMSO; insoluble in EtOH |
| Canonical SMILES | CC(O)=O.CC.CC.CCccC.[R].[P].[2H].[L].[E].[P].[P].[Y].[3H].[G].[KH].[R].[R].[Y].F.[Y].[*].[L].F.[V].[Y].[G].[G].[R].[KH].[R].N.N.F.[KH].S.[*].[2H].[R].[G].[G].[*].[KH].[*].[3H].C.[*].F.[P].[*].I.I.N.[Q].[3H].[M] |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment: [1] | |
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Cell lines |
HUVEC cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
1600 kIU/mL, 60 min |
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Applications |
Aprotinin dose-dependently inhibited the TNF-α–induced expression of ICAM-1 and VCAM-1, but not E-selectin. |
| Animal experiment : [2] | |
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Animal models |
3- to 4-mo-old male Albino Wistar rats |
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Dosage form |
The rats were anesthetized by 50 mg/kg of ketamine initially and treated with 12 mmHg pneumoperitoneum for 4 h. Additional lower doses of ketamine were administered i.p. until the end of pneumoperitoneum to maintain anesthesia. A loading aprotinin dose of 28000 KIU/kg was given i.p. after the onset of pneumoperitoneum, followed by lower maintenance doses (7500 KIU/kg), which were administered per hour until the termination. Splanchnic reperfusion period lasted 60 or 180 min. |
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Applications |
Treatment of aprotinin caused reduction of several cytokines and markers (TNF-α, IL-6, endothelin 1, C reactive protein, PAB and carbonyl proteins) of oxidative stress in all tissues (liver, small intestine, and lung) studied. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Asimakopoulos G, Lidington E A, Mason J, et al. Effect of aprotinin on endothelial cell activation. The Journal of thoracic and cardiovascular surgery, 2001, 122 (1): 123-128. [2] Baltatzis M, Pavlidis T E, Ouroumidis O, et al. Aprotinin reduces oxidative stress induced by pneumoperitoneum in rats. Journal of Surgical Research, 2014, 189 (2): 238-248. |
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| Description | Aprotinin is the small protein bovine pancreatic trypsin inhibitor (BPTI). | |||||
| Targets | bovine pancreatic trypsin | |||||
| IC50 | ||||||
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
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