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Cyclosporin A (Synonyms: Cyclosporine; Ciclosporin)

Cat. No.: HY-B0579 Purity: >98.0%
Data Sheet SDS Handling Instructions

Cyclosporin A is an immunosuppressive agent, that binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay, and is widely used in organ transplantation to prevent rejection.

For research use only. We do not sell to patients.
Cyclosporin A Chemical Structure

Cyclosporin A Chemical Structure

CAS No. : 59865-13-3

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
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200 mg $70 In-stock
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Customer Review

    Cyclosporin A purchased from MCE. Usage Cited in: Environ Sci Technol. 2017 Nov 9.

    Cellular staining with Fluo-3/AM, Rhod-2 and DAPI (blue) in cells upon nLa2O3 treatment at 20 μg/mL for 6 h. Cells are examined with confocal microscopy. Two colors are showed individually or merged together.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Cyclosporin A is an immunosuppressive agent, that binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay, and is widely used in organ transplantation to prevent rejection.

    IC50 & Target

    IC50: 7 nM (calcineurin)

    In Vitro

    Cyclosporin A binds to the cyclophilin (immunophilin) in T cells[1], and forms a Cyclophilin-Cyclosporin A complex which inhibits calcineurin[2]. Cyclosporin A inhibits calcineurin with IC50 of 7 nM[3], then blocks the nuclear translocation of NF-AT[4]. Cyclosporin A also affects mitochondria by preventing the MTP (mitochondrial permeability transition pore) from opening with an IC50 of 39 nM[5]

    In Vivo

    Cyclosporin A is an immunosuppressive agent that is effective following either parenteral or oral administration in mice, rat and guinea pigs[6]. Cyclosporin A is clinically used in organ transplantation to prevent rejection[7]

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume 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
    Please refer to the solubility information to select the appropriate solvent.
    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]

    Cyclosporin A is dissolved in ethanol.

    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]

    Cyclosporin A is suspended in 0.5% solution of tragacanth.

    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
    Molecular Weight

    1202.61

    Formula

    C₆₂H₁₁₁N₁₁O₁₂

    CAS No.

    59865-13-3

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    Cyclosporin A
    Cat. No.:
    HY-B0579
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