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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Aprotinin 構造式

Aprotinin 構造式

CAS 番号 : 9087-70-1

容量 価格(税別) 在庫状況 数量
5 mg USD 50 在庫あり
10 mg USD 80 在庫あり
25 mg USD 160 在庫あり
50 mg USD 250 在庫あり
100 mg USD 400 在庫あり
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カスタマーレビュー

Based on 15 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.
    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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]

    体外実験

    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.

    体内実験

    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.

    臨床実験
    分子量

    6511.44

    分子式

    C284H432N84O79S7

    CAS 番号
    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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

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

    溶剤 & 溶解度
    体外: 

    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
    10 mM 0.0154 mL 0.0768 mL 0.1536 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.

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    体内:

    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

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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    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).
    純度とドキュメンテーション

    純度: 99.01%

    参考文献
    動物実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

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

    一般には略語で表示されます:C1V1 = C2V2

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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

    製品名:
    Aprotinin
    製品番号:
    HY-P0017
    数量:
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