Home Metabolism phosphatase inhibitor - Immunology & Inflammation related inhibitor Cyclosporine For research use only.

Cyclosporine

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

Cyclosporine Chemical Structure

Cyclosporine Chemical Structure

CAS No. 79217-60-0

Purity & Quality Control

Cyclosporine Related Products

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05702931 Not yet recruiting
Hyperglycemia|Renal Transplant Complication Primary Non-Function|Diabetes
Rigshospitalet Denmark|Aarhus University Hospital|Odense University Hospital
 April 1 2024 Phase 4
NCT05955924 Recruiting
Non-melanoma Skin Cancer|Carcinoma Squamous Cell|Carcinoma Basal Cell|Keratinocyte Carcinoma
Women''s College Hospital|Canadian Institutes of Health Research (CIHR)|University Health Network Toronto|NOW Foods
 August 28 2023 Phase 3
NCT04989686 Recruiting
Immunosuppression
Children''s Hospital of Philadelphia|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)
 June 8 2023 --
NCT05745701 Completed
Healthy
Pfizer
 February 22 2023 Phase 1
NCT05056779 Withdrawn
Moderate-to-severe Atopic Dermatitis
Galderma R&D
 January 2023 Phase 3

Chemical Information & Solubility

Molecular Weight 1202.61 Formula

C62H111N11O12
CAS No. 79217-60-0 SDF Download Cyclosporine SDF
Smiles CCC1C(=O)N(CC(=O)N(C(C(=O)NC(C(=O)N(C(C(=O)NC(C(=O)NC(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N1)C(C(C)CC=CC)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (83.15 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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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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