Cyclosporine

Catalog No.S1514

Cyclosporine  Chemical Structure

Molecular Weight(MW): 1202.61

Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.

Size Price Stock Quantity  
In DMSO USD 480 In stock
USD 120 In stock
USD 370 In stock
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Biological Activity

Description Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.
Targets
calcineurin phosphatase [2]
In vitro

Cyclosporine induces phenotypic changes, including invasiveness of non-transformed cells, by a cell-autonomous mechanism. Cyclosporine treatment of adenocarcinoma cells results in striking morphological alterations, including membrane ruffling and numerous pseudopodial protrusions, increased cell motility, and anchorage-independent (invasive) growth. [1] Cyclosporine (cyclosporin A, CsA) has potent immunosuppressive properties, reflecting its ability to block the transcription of cytokine genes in activated T cells. Cyclosporine through formation of a complex with cyclophilin inhibits the phosphatase activity of calcineurin, which regulates nuclear translocation and subsequent activation of NFAT transcription factors. Cyclosporine also blocks the activation of JNK and p38 signaling pathways triggered by antigen recognition, making CsA a highly specific inhibitor of T cell activation. [2] Cyclosporine-mediated inhibition of the biliary excretion of MPAG by the Mrp2 transporter is the mechanism responsible for the interaction between Cyclosporine and mycophenolate mofetil (MMF). [3] Cyclosporine inhibits biochemical and morphological differentiation of skeletal muscle cells while having a minimal effect on proliferation. [4]

In vivo Cyclosporine enhances tumour growth in immunodeficient SCID-beige mice. [1] Cyclosporine inhibits muscle regeneration after induced trauma in mice. [4] Cyclosporine peaks at 1 hour in blood, spleen, and kidney, with higher concentrations in spleen and kidney than in blood. [5]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (83.15 mM)
Ethanol 100 mg/mL (83.15 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
3mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1202.61
Formula

C62H111N11O12

CAS No. 79217-60-0
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04023760 Recruiting Drug: Apixaban Pharmacokinetics|Kidney Transplant|Lung Transplant University of Saskatchewan|Saskatchewan Health Research Foundation|Lung Association of Saskatchewan June 26 2019 Phase 4
NCT03750383 Completed Drug: EDP-938|Drug: Cyclosporine|Drug: Prednisone RSV Infection Enanta Pharmaceuticals|Pharmaceutical Research Associates November 2 2018 Phase 1
NCT03865888 Completed Drug: Cyclosporins|Drug: Tacrolimus Dry Eye|Sjogren Syndrome Pavly Moawd|Cairo University October 30 2018 Phase 3
NCT02998645 Recruiting Drug: eltrombopag|Drug: Cyclosporine Severe Aplastic Anemia Novartis Pharmaceuticals|Novartis May 11 2017 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    What is the difference between S2286 (cyclosporin A) and S1514 (cyclosporin)?

  • Answer:

    Cyclosporine is a mixture of Cyclosporine A, derivatives of Cyclosporine A, salts of Cyclosporine A. Cyclosporine A is an especially useful Cyclosporine component.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID