1. Anti-infection Metabolic Enzyme/Protease
  2. Influenza Virus Ser/Thr Protease
  3. Aprotinin

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

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No. CAS : 9087-70-1

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Revisión del cliente

Based on 31 publication(s) in Google Scholar

Top Publications Citing Use of Products

31 Publications Citing Use of MCE Aprotinin

WB

    Aprotinin purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Mar 27;43(4):114002.  [Abstract]

    A431 cells were treated with EGF (10 ng/mL) together with Aprotinin (2 μM) for 1 h. Proteins were detected by western blots.

    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.
    • Actividad biológica

    • Protocolo

    • Pureza y Documentación

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    • Revisión del cliente

    Descripciòn

    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.

    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.

    Ensayo clínico
    Peso molecular

    6511.44

    Fòrmula

    C284H432N84O79S7

    No. CAS
    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
    Initial Source

    Bovine lung

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Solvente y solubilidad
    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
    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.

    • Calculadora de molaridad

    • Calculadora de dilución

    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).
    Pureza y Documentación

    Referencias
    Administraciòn de animales
    [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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

    Referencias

    Complete Stock Solution Preparation Table

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    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
    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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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Inquiry Information

    Nombre del producto:
    Aprotinin
    Cat. No.:
    HY-P0017
    Cantidad:
    MCE Japan Authorized Agent: