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  3. Aprotinin

Aprotinin 

Cat. No.: HY-P0017 Purity: >98.0%
Handling Instructions

Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively.

For research use only. We do not sell to patients.

Aprotinin Chemical Structure

Aprotinin Chemical Structure

CAS No. : 9087-70-1

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Aprotinin purchased from MCE. Usage Cited in: Am J Physiol Cell Physiol. 2017 Dec 1;313(6):C632-C643.

    Effects of protease inhibitor PIC, a serine protease inhibitor AEBSF and trypsin and chymotrypsin inhibitors Aprotinin (Aprot, 0.1 mM) on PRR cleavage induced by BSA in HK-2 cells.
    • Biological Activity

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    Description

    Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively.

    IC50 & Target

    Ki: 0.06 pM (Trypsin), 9 nM (Chymotrypsin)[1]

    In Vitro

    Aprotinin, a serine protease inhibitor isolated from bovine lung, is a complex protease inhibitor that is an antifibrinolytic, inhibits contact activation, and decreases the inflammatory response to cardiopulmonary bypass[2]. Aprotinin inhibits trypsin (bovine, Ki= 0.06 pM), chymotrypsin (bovine, Ki= 9 nM), plasmin (human, 0.23 nM)[1]. 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[3]. Aprotinin significantly inhibits fibrinolysis with an IC50 of 0.16±0.05 μM[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    High dose aprotinin can reduce blood loss and transfusion requirements associated with primary cardiac procedures such as coronary artery bypass graft (CABG) or heart valve replacement surgery[5]. Aprotinin inhibits thrombus formation in a dose-dependent manner. Aprotinin at a dose of 1.5 mg kg-1 (bolus) and 3 mg kg-1 h-1 infusion (maintenance infusion) causes a tendency towards a reduction in bleeding time. Aprotinin significantly reduces the bleeding time starting at a dose of 3 mg kg-1 bolus plus 6 mg kg-1 h-1 showing a reduction of approximately 84%±2.9%. At the highest dose of 5 mg kg-1 and 10 mg kg-1 h-1, the strongest effects are observed[4]. Aprotinin may affect tumor necrosis factor-alpha (TNF) levels. Soluble TNFRI levels are significantly increased following I/R in the aprotinin treated wild type mice and not detected in all TNFRInull mice[6].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    6511.44

    Formula

    C₂₈₄H₄₃₂N₈₄O₇₉S₇

    CAS No.

    9087-70-1

    Sequence

    Arg-Pro-Asp-Phe-Cys-Leu-Glu-Pro-Pro-Tyr-Thr-Gly-Pro-Cys-Lys-Ala-Arg-Ile-Ile-Arg-Tyr-Phe-Tyr-Asn-Ala-Lys-Ala-Gly-Leu-Cys-Gln-Thr-Phe-Val-Tyr-Gly-Gly-Cys-Arg-Ala-Lys-Arg-Asn-Asn-Phe-Lys-Ser-Ala-Glu-Asp-Cys-Met-Arg-Thr-Cys-Gly-Gly-Ala

    Sequence Shortening

    RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA

    SMILES

    [RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -80°C 2 years
    -20°C 1 year
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (15.36 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.1536 mL 0.7679 mL 1.5358 mL
    5 mM 0.0307 mL 0.1536 mL 0.3072 mL
    10 mM 0.0154 mL 0.0768 mL 0.1536 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Animal Administration
    [4][6]

    Rats: Male Wistar rats (180-220 g) are used in the study. Aprotinin is dissolved in physiological saline. Aprotinin is administered by bolus injection followed by a maintenance infusion. The doses given are 1.5 mg kg-1 and 3 mg kg-1 h-1, 3mg kg-1 and 6 mg kg-1 h-1 up to 5 mg kg-1 and 10 mg kg-1 h-1. Plasma concentrations for the two agents are assessed by pharmacokinetic studies in rats[4].

    Mice: An intact mouse model of ischemia/reperfusion (30 min-I/60 min-R) is used and left ventricular peak + dP/dt is measured in wild type mice (WT, C57BL/6; n=10), WT mice with aprotinin (4mL/kg; n=10), transgenic mice devoid of the TNFRI (TNFRInull; n=10), and TNFRInull with aprotinin (n=10)[6].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: >98.0%

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    Keywords:

    AprotininInfluenza VirusInhibitorinhibitorinhibit

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    Product Name:
    Aprotinin
    Cat. No.:
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