Aprotinin

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 Chemical Structure

Aprotinin Chemical Structure

CAS: 9087-70-1

Selleck's Aprotinin has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.81%
99.81

Choose Selective Serine Protease Inhibitors

Biological Activity

Description Aprotinin is a small protein serine protease inhibitor (Kd=0.06 pM for bovine β-trypsin), used to reduce perioperative blood loss and transfusion.
Targets
Thrombin [1]
(Cell-free assay)
Trypsin [1]
(Cell-free assay)
kallikrein [1]
(Cell-free assay)
chymotrypsin [1]
(Cell-free assay)
trypsinogen [1]
(Cell-free assay)
0.06 pM(Kd) 0.8 nM(Kd) 9.5 nM(Kd) 2 μM(Kd)
In vitro
In vitro Aprotinin is an antifibrinolytic molecule that inhibits trypsin and related proteolytic enzymes. In cell biology, aprotinin is used as an enzyme inhibitor to prevent protein degradation during lysis or homogenization of cells and tissues. In the presence of aprotinin, the fibrinolytic activity is inhibited concentration dependently and the coagulation time is prolonged. Aprotinin is an effective inhibitor of the contact (intrinsic) coagulation pathway in vitro[2].
Cell Research Cell lines mouse G8-1 and C2C12 skeletal muscle myoblasts
Concentrations 2 TIU/ml
Incubation Time 12hrs
Method

Mouse G8-1 myoblasts are plated DMEM + 20% FBS (maintenance medium), in which they remain undifferentiated. When cells reach approximately 40-50% confluence, different protease inhibitors are added to the culture media and cells are incubated overnight. Cells are then switched to differentiation-promoting media (DMEM + 10% horse serum ± protease inhibitor) and incubated for 7 days.

In Vivo
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, aprotinin reduces thrombus weight [2].
Animal Research Animal Models Male Wistar rats
Dosages 1.5 mg/kg and 3 mg/kg/h, 3 mg/kg and 6 mg/kg/h up to 5 mg/kg and 10 mg/kg/h
Administration bolus injection followed by a maintenance infusion(i.p.)
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

Chemical lnformation & Solubility

Molecular Weight 6511.51 Formula

C284H432N84O79S7

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

In vitro
Batch:

Water : 100 mg/mL


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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