Home Proteases Serine Protease inhibitor Aprotinin

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Aprotinin Protease Inhibitor

Cat.No.S7377

Aprotinin is a small protein serine protease inhibitor (Kd=0.06 pM for bovine β-trypsin), used to reduce perioperative blood loss and transfusion.
Aprotinin Serine Protease inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 6511.51

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 6511.51 Formula

C284H432N84O79S7

 Storage (From the date of receipt)
CAS No. 9087-70-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCC(C)C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC2CSSCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)N4CCCC4C(=O)N5CCCC5C(=O)NC(C(=O)NC(C(=O)NCC(=O)N6CCCC6C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N3)CC(=O)O)CCC(=O)O)C)CO)CCCCN)CC7=CC=CC=C7)CC(=O)N)CC(=O)N)CCCNC(=N)N)CCCCN)C)CCCNC(=N)N)NC(=O)CNC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC2=O)CCC(=O)N)C(C)O)CC8=CC=CC=C8)C(C)C)CC9=CC=C(C=C9)O)C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCNC(=N)N)C)CCCCN)C(C)O)CC1=CC=C(C=C1)O)CCC(=O)O)CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C(CC(=O)O)NC(=O)C1CCCN1C(=O)C(CCCNC(=N)N)N)C(=O)NCC(=O)NCC(=O)NC(C)C(=O)O)C(C)O)CCCNC(=N)N)CCSC)CC(C)C)C)CCCCN)C)CC(=O)N)CC1=CC=C(C=C1)O)CC1=CC=CC=C1)CC1=CC=C(C=C1)O)CCCNC(=N)N)C(C)CC

Solubility

In vitro
Batch:

Water : 100 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Thrombin [1]
(Cell-free assay)
Trypsin [1]
(Cell-free assay)
0.06 pM(Kd)
kallikrein [1]
(Cell-free assay)
0.8 nM(Kd)
chymotrypsin [1]
(Cell-free assay)
9.5 nM(Kd)
trypsinogen [1]
(Cell-free assay)
2 μM(Kd)
In vitro
Aprotinin is an antifibrinolytic molecule that inhibits trypsin and related proteolytic enzymes. In cell biology, this compound is used as an enzyme inhibitor to prevent protein degradation during lysis or homogenization of cells and tissues. In the presence of this inhibitor, the fibrinolytic activity is inhibited concentration dependently and the coagulation time is prolonged. It is an effective inhibitor of the contact (intrinsic) coagulation pathway in vitro[2].
In vivo
Aprotinin inhibits clot lysis in vitro as well as rat-tail bleeding time in vivo and prolongs coagulation time in human plasma. In a rat arteriovenous shunt model, this compound reduces thrombus weight [2].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00481806 Unknown status
Coronary Artery Bypass|Thrombosis
University of Arizona|University of Maryland Baltimore County
 February 2007 --
NCT00354900 Terminated
Metastatic Breast Cancer
Dartmouth-Hitchcock Medical Center
 July 2006 Phase 1
NCT00131040 Completed
Ischemic Heart Disease|Angina Pectoris
Imperial College London|British Heart Foundation
 January 2003 Not Applicable

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