Hot Sell Ciclosporin A Cyclosporin CAS 59865-13-3

Details:

Synonyms Name: Cyclosporine       

CAS No.: 59865-13-3

Molecular Formula: C62H111N11O12

Cyclosporine or cyclosporine A, is an immunosuppressant drug. Cyclosporine widely used in post-allogeneic organ transplant to reduce the activity of the patient's immune system, and therefore the risk of organ rejection. Cyclosporine has been studied in transplants of skin, heart, kidney, liver, lung, pancreas, bone marrow, and small intestine. Cyclosporine initially isolated from the fungus Tolypocladium inflatum isolated from a soil, ciclosporine is a cyclicnonribosomal peptide of 11 amino acids and contains a single D-amino acid, which are rarely encountered in nature.

Cyclosporine is thought to bind to the cytosolic protein cyclophilin(immunophilin) of immunocompetent lymphocytes, especially T-lymphocytes. This complex of ciclosporin and cyclophilin inhibits calcineurin, which, under normal circumstances, is responsible for activating the transcription of interleukin 2. In T-cells, activation of the T-cell receptor normally increases intracellular calcium, which acts via calmodulin to activate calcineurin. Calcineurin then dephosphorylates the transcription factor NF-AT (nuclear factor of activated T-cells), which moves to the nucleus of the T-cell and increases the activity of genes coding for IL-2 and related cytokines. Ciclosporin prevents the dephosphorlyation of NF-AT by binding to cyclophilin.[7] It also inhibits lymphokine production andinterleukin release and, therefore, leads to a reduced function of effector T-cells. It does not affect cytostaticactivity.

It also has an effect on mitochondria. Ciclosporine prevents the mitochondrial permeability transition pore from opening, thus inhibiting cytochrome c release, a potent apoptotic stimulation factor. However, this is not the primary mechanism of action for clinical use, but rather an important effect for research on apoptosis.

 

 

   

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