SKU: C092

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Description

Cyclosporin, USP is a mixture of cyclic oligopeptide immunosuppressant compounds routinely given to patients after receiving an organ transplant to prevent transplant rejection. Cyclosporin, USP contains mostly cyclosporin A (>98.0%) which has the most potent immunosuppressant activity of the cyclosporins and is highly metabolized by humans and animals after ingestion. The resulting metabolites (cyclosporin B, C, D, E, H, L, and others) have been found to have less potent immunosuppressant activity and are associated with higher nephrotoxicity when compared to cyclosporin A.

TOKU-E offers purified forms of cyclosporin A, B, C, D, E, H, and L.

    CAS Number

    59865-13-3

    Molecular Formula

    C62H111N11O12

    Molecular Weight

    1202.61

    Mechanism of Action

    Cyclosporin A (CsA) immunosuppressant activity stems from its ability to prevent T-cell activation by blocking specific cytokine transcription genes. After entering a T-cell, cyclosporin A (CsA) associates with ubiquitous cytosolic proteins called cyclophilins which aid in protein folding. Cyclosporin A (CsA) : cyclophilin complexes together bind calcineurin, (another cytosolic protein) effectively blocking the pathway to IL-2 gene transcription and nitric oxide synthesis by TNFα and interleukin 1α.

    Storage Conditions

    2-8 °C

Applications

    Cancer Applications

    Cyclosporins can be used to study toxicity and immunosuppressant activity in various in vitro assays and experiments.

Specifications

    Form

    Powder

    Appearance

    White crystalline powder

    Assay

    98.5-101.5% (on dried basis)

    Loss on Drying

    ≤2.0%

    Heavy Metals

    ≤0.002%

    Impurities

    Related Compounds:
    Individual impurity: ≤0.7%
    Total impurities: ≤1.5%

References

    References

    Stiller, C. R., MD, and R. A. Ulan, MD. "Cyclosporin A: A Powerful Immunosuppressant."Canadian Medical Association 126 (1981): 1041-046. www.ncbi.gov. Web. 27 Aug. 2012.

    Crabtree, G. R., J. Nourse, and L. Timmermann. "The Mechanism of Action of Cyclosporin A and FK506." Clinical Immunology and Immunotherapy (1996): 40-45.www.ncbi.gov. Web. 27 Aug. 2012.

    Wang, Paul C. et. al. "Isolation of 10 Cyclosporine Metabolites from Human Bile." Drug Metabolism and Disposition 17.3 (1989): 292-96. Nih.gov. Web. 28 Oct. 2013.

    Copeland, Kenneth R. "Immunosuppressive Activity of Cyclosporine Metabolites Compared and Characterized by Mass Spectrometry and Nuclear Magnetic Resonance."Clinical Chemistry 36.2 (1990): 225-29. Web. 28 Oct. 2013.

    Matsuda, Staoshi. "Mechanisms of Action of Cyclosporine." Immunopharmacology 47 (2000): 119-25. Elsevier. Web. 28 Oct. 2013.

    Laupacis, A., and P. A. Keown. "Cyclosporin A: A Powerful Immunosuppressant." Therapeutic Review 126 (1982): 1041-046. Nih.gov. Web. 6 Nov. 2013.

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