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> Aprotinin [9087-70-1]

Aprotinin [9087-70-1]

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Cat# HY-P0017-10mg

Size : 10mg

Brand : MedChemExpress

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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

This product is a controlled substance and not for sale in your territory.

Based on 15 publication(s) in Google Scholar

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

    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.
    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].

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

    Aprotinin Related Antibodies
    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].

    MedChemExpress (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
    Appearance

    Solid

    Color

    Off-white to light brown

    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(Disulfide bridge: Cys5-Cys55,Cys14-Cys38,Cys30-Cys51)
    Sequence Shortening

    RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA(Disulfide bridge: Cys5-Cys55,Cys14-Cys38,Cys30-Cys51)
    SMILES

    O=C(N1[C@@H](CCC1)C(N[C@@H](CC(O)=O)C(N[C@@H](CC2=CC=CC=C2)C(N[C@@H](CSSC[C@@H](C(NCC(NCC(N[C@@H](C)C(O)=O)=O)=O)=O)NC3=O)C(N[C@@H](CC(C)C)C(N[C@@H](CCC(O)=O)C(N4[C@@H](CCC4)C(N5[C@@H](CCC5)C(N[C@@H](CC6=CC=C(C=C6)O)C(N[C@@H]([C@H](O)C)C(NCC(N7[C@@H](CCC7)C(N[C@@H](CSSC[C@@H](C(N[C@H](CCCNC(N)=N)C(N[C@@H](C)C(N[C@@H](CCCCN)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(N)=O)C(N[C@@H](CC(N)=O)C(N[C@@H](CC8=CC=CC=C8)C(N[C@@H](CCCCN)C(N[C@@H](CO)C(N[C@@H](C)C(N[C@@H](CCC(O)=O)C(N[C@H]9CC(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)NC%10=O)C(N[C@@H](CCCCN)C(N[C@@H](C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H]([C@@H](C)CC)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC%11=CC=C(C=C%11)O)C(N[C@@H](CC%12=CC=CC=C%12)C(N[C@@H](CC%13=CC=C(C=C%13)O)C(N[C@@H](CC(N)=O)C(N[C@@H](C)C(N[C@@H](CCCCN)C(N[C@@H](C)C(NCC(N[C@@H](CC(C)C)C(N[C@@H](CSSC[C@@H](C(N[C@@H](CCSC)C(N[C@@H](CCCNC(N)=N)C(N[C@H]3[C@H](O)C)=O)=O)=O)NC9=O)C(N[C@@H](CCC(N)=O)C(N[C@@H]([C@H](O)C)C(N[C@@H](CC%14=CC=CC=C%14)C(N[C@@H](C(C)C)C(N[C@@H](CC%15=CC=C(C=C%15)O)C(NCC(NC%10)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CCCNC(N)=N)N
    Structure Classification
    • Others
    Initial Source
    • Animals

    Bovine lung
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Solvent & Solubility
    In Vitro: 

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

    DMSO : 66.67 mg/mL (10.24 mM; ultrasonic and adjust pH to 3 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL (7.68 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.01%

    SDS (393 KB)

    COA (230 KB) RP-HPLC (475 KB) MS (530 KB)

    Handling Instructions (2659 KB)
    References

    • [1]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62.  [Content Brief]

      [2]. Fritz H, et al. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94.  [Content Brief]

      [3]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62.

      [4]. Venturini G, et al. Aprotinin, the first competitive protein inhibitor of NOS activity. Biochem Biophys Res Commun. 1998 Aug 10;249(1):263-5  [Content Brief]

      [5]. Sperzel M, et al. 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. Epub 2007 Jul 31.  [Content Brief]

      [6]. Davis R, et al. Aprotinin. A review of its pharmacology and therapeutic efficacy in reducing blood loss associated withcardiac surgery. Drugs. 1995 Jun;49(6):954-83.  [Content Brief]

      [7]. Sabbagh MJ, et al. Aprotinin exacerbates left ventricular dysfunction after ischemia/reperfusion in mice lacking tumor necrosis factor receptor I. J Cardiovasc Pharmacol. 2008 Oct;52(4):355-62.  [Content Brief]

    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

    • [1]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62.  [Content Brief]

      [2]. Fritz H, et al. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94.  [Content Brief]

      [3]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62.

      [4]. Venturini G, et al. Aprotinin, the first competitive protein inhibitor of NOS activity. Biochem Biophys Res Commun. 1998 Aug 10;249(1):263-5  [Content Brief]

      [5]. Sperzel M, et al. 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. Epub 2007 Jul 31.  [Content Brief]

      [6]. Davis R, et al. Aprotinin. A review of its pharmacology and therapeutic efficacy in reducing blood loss associated withcardiac surgery. Drugs. 1995 Jun;49(6):954-83.  [Content Brief]

      [7]. Sabbagh MJ, et al. Aprotinin exacerbates left ventricular dysfunction after ischemia/reperfusion in mice lacking tumor necrosis factor receptor I. J Cardiovasc Pharmacol. 2008 Oct;52(4):355-62.  [Content Brief]

    • [1]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62.

      [2]. Fritz H, et al. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94.

      [3]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62.

      [4]. Venturini G, et al. Aprotinin, the first competitive protein inhibitor of NOS activity. Biochem Biophys Res Commun. 1998 Aug 10;249(1):263-5

      [5]. Sperzel M, et al. 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. Epub 2007 Jul 31.

      [6]. Davis R, et al. Aprotinin. A review of its pharmacology and therapeutic efficacy in reducing blood loss associated withcardiac surgery. Drugs. 1995 Jun;49(6):954-83.

      [7]. Sabbagh MJ, et al. Aprotinin exacerbates left ventricular dysfunction after ischemia/reperfusion in mice lacking tumor necrosis factor receptor I. J Cardiovasc Pharmacol. 2008 Oct;52(4):355-62.

    Complete Stock Solution Preparation Table

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 0.1536 mL 0.7679 mL 1.5358 mL 3.8394 mL
    5 mM 0.0307 mL 0.1536 mL 0.3072 mL 0.7679 mL
    10 mM 0.0154 mL 0.0768 mL 0.1536 mL 0.3839 mL
    H2O 15 mM 0.0102 mL 0.0512 mL 0.1024 mL 0.2560 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Aprotinin Related Classifications

    • Enzyme
    • Protease
    • Cardiovascular Disease Cancer
    • Cancer Targeted Therapy Cancer Immunotherapy Cancer Metabolism and Metastasis
    • Anti-infection Metabolic Enzyme/Protease
    • Influenza Virus Ser/Thr Protease
    Help & FAQs

    Keywords:

    Aprotinin9087-70-1Influenza VirusSer/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasesInhibitorinhibitorinhibit

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