1. Cyclosporin A

Cyclosporin A (Synonyms: Cyclosporine; Ciclosporin)

目录号: HY-B0579 纯度: >98。0%

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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    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.
    • 生物活性

    • 实验参考方法

    • 技术信息

    • 纯度 & 产品资料

    • 参考文献


    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

    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)

    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

    • 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。
    • [1].







    Kinase Assay

    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

    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

    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.

    • [1].







    Molecular Weight




    CAS No.





    Room temperature in continental US; may vary elsewhere

    Purity: >98.0%

    • [1].







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    Cyclosporin A

    Cyclosporin A

    Cat. No.: HY-B0579

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