1. Cyclosporin A

Cyclosporin A (Synonyms: Cyclosporine; Ciclosporin)

目录号: HY-B0579 纯度: >98。0%
产品使用指南

Cyclosporin A 是一种免疫抑制剂,能与亲环素结合,抑制 calcineurin 活性的IC50 值为 7 nM。

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Cyclosporin A Chemical Structure

Cyclosporin A Chemical Structure

CAS No. : 59865-13-3

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MCE 顾客使用本产品发表的科研文献

    Cyclosporin A purchased from MCE. Usage Cited in:

    A549 cells are pretreated with 5 µM Cyclosporin A (CSA) for 2 h, followed by treatment with 80 μM Hirsutine for 24 h. equal amount of lysates are subjected to immunoprecipitation using anti-ANT1 antibody, the associated CypD is determined using immunoblotting.
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    • 参考文献

    Description

    Cyclosporin A is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM.

    IC50 & Target

    IC50: 7 nM (calcineurin)

    In Vitro

    Cyclosporin A is able to bind with the cyclophilin in T cells[1]. Cyclosporin A works by forming a Cyclophilin-Cyclosporin A complex to inhibit calcineurin[2]. Cyclosporin A exhibits inhibitory effect on calcineurin with an IC50 of 7 nM[3]. Cyclosporin A suppresses the nuclear translocation of NF-AT[4]. Cyclosporin A shows an effect on mitochondria via preventing the MTP from opening with an IC50 of 39 nM[5].

    In Vivo

    Cyclosporin A has immunosuppressive activity, and is active via parenteral and p.o. administration in mice, rat and guinea pigs[6]. Cyclosporin A can be used in organ transplantation to prevent rejection[7].

    Clinical Trial
    Storage

    4°C, protect from light

    Solvent & Solubility
    In Vitro: 

    DMSO : 62.5 mg/mL (51.97 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.8315 mL 4.1576 mL 8.3152 mL
    5 mM 0.1663 mL 0.8315 mL 1.6630 mL
    10 mM 0.0832 mL 0.4158 mL 0.8315 mL
    * 请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存方式和期限。
    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案,配制前请先配制澄清的储备液,再依次添加助溶剂 (为保证实验结果的可靠性,体内实验的工作
    液,建议您现用现配,当天使用;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分比是指该溶剂在您配制终溶液中的体积占比):

    • 1.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2。08 mg/mL (1。73 mM); Clear solution

    • 2.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.08 mg/mL (1.73 mM); Suspended solution; Need ultrasonic

    *以上所有助溶剂都可在 MCE 网站选购。
    References
    • [1].

      [2].

      [3]。

      [4]。

      [5].

      [6]。

      [7].

    Kinase Assay
    [3]

    Reaction mixtures with purified enzyme contains 100 nM calcineurin, 100 nM calmodulin, and 5 μM 32P-labeled phosphopeptide, in 60 μL (total volume) of assay buffer containing 20 mM Tris (pH 8), 100 mM NaCl, 6 mM MgCl2, 0.5 mM dithiothreitol, 0.1 mg of bovine serum albumin per mL, and either 0.1 mM CaCl2 or 5 mM EGTA. Reaction mixtures with cell lysates contains 20 μL of undiluted lysate, 5 μM 32P-labeled phosphopeptide, and 40 μL of assay buffer. Reaction mixtures contains 50 μM peptide 412 or 413 and/or 500 nM okadaic acid, a specific inhibitor of phosphatases 1 and 2A; 500 nM okadaic acid is sufficient for inhibition of Ca2+-independent phosphatases, whereas higher concentrations partially inhibit Ca2+-dependent activity as well. After 15 min at 30°C, reactions are terminated by the addition of 0.5 mL of 100 mM potassium phosphate buffer (pH 7.0) containing 5% trichloroacetic acid. Free inorganic phosphate is isolated by Dowex cation-exchange chromatography and quantitated by scintillation counting as described.

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

    Cell Assay
    [3]

    Immunosuppressive agents are dissolved in ethanol at concentrations 1000-fold more than the concentration desired for cell treatments. Cells (106) are suspended in 1 mL of complete medium in microcentrifuge tubes; 1 μL of ethanol or of the ethanolic solution of Cyclosporin A is added, and the cells are incubated at 37°C for 1 hr. Cells are washed twice with 1 mL of PBS on ice and lysed in 50 μL of hypotonic buffer containing 50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM dithiothreitol; and 50 μg of phenylmethylsulfonyl fluoride, 50 μg of soybean trypsin inhibitor, 5 μg of leupeptin, and 5 μg of aprotinin per mL. Lysates are subjected to three cycles of freezing in liquid nitrogen followed by thawing at 30°C and then are centrifuged at 4°C for 10 min at 12,000×g.

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

    Animal Administration
    [6]

    Rats are immunized on day 0 i.p. with 0 5 mL and mice i.v. with 0 2 mL of a 10% suspension of washed sheep erythrocytes (SE). To elicit a secondary response, mice are boosted 8-11 weeks after the primary immunization with an i.v. injection of 0-2 mL of 0 25% washed SE (107 cells). For prolonged treatment the animals receive on the average 45 mg/kg cyclosporin A daily in the food during 13 weeks. These rats are immunized 5 days before killing.

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

    References
    • [1].

      [2].

      [3].

      [4].

      [5].

      [6].

      [7].

    Molecular Weight

    1202.61

    Formula

    C₆₂H₁₁₁N₁₁O₁₂

    CAS No.

    59865-13-3

    SMILES

    O[C@@H]([C@](C(N[C@H](C(N(CC(N([C@H](C(N[C@@](C(N([C@H]1CC(C)C)C)=O)([H])C(C)C)=O)CC(C)C)C)=O)C)=O)CC)=O)([H])N(C([C@](N(C([C@@H](N(C([C@H](N(C([C@H](NC([C@@H](NC1=O)C)=O)C)=O)C)CC(C)C)=O)C)CC(C)C)=O)C)([H])C(C)C)=O)C)[C@H](C)C/C=C/C

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: >98.0%

    • [1].

      [2].

      [3].

      [4].

      [5].

      [6].

      [7]。

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    产品名称:
    Cyclosporin A
    目录号:
    HY-B0579
    需求量:

    Cyclosporin A

    Cat. No.: HY-B0579

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