Catalog No.S2286 Synonyms: Cyclosporine A
Molecular Weight(MW): 1202.61
Cyclosporin A is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay, widely used in organ transplantation to prevent rejection.
Cited by 24 Publications
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|Description||Cyclosporin A is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay, widely used in organ transplantation to prevent rejection.|
Cyclosporin A binds to the cyclophilin (immunophilin) in T cells , forms a Cyclophilin-Cyclosporin A complex which the binds to and inhibits calcineurin.  Cyclosporin A inhibits calcineurin with IC50 of 7 nM, then blocks the nuclear translocation of NF-AT.  Cyclosporin A also affects mitochondria by preventing the MTP (mitochondrial permeability transition pore) from opening with an IC50 of 39 nM. 
|In vivo||Cyclosporin A is an immunosuppressive agent that is effective following either parenteral or oral administration in mice, rat and guinea pigs. , is clinically used in organ transplantation to prevent rejection. |
Phosphatase Assay:Purified bovine brain calcineurin and calmodulin are purchased. 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 NaCI, 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. Where indicated, 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.
-  Handschumacher RE, et al. Science, 1984, 226(4674), 544-547.
-  Liu J, et al. Cell, 1991, 66(4), 807-815.
-  Fruman DA, et al. PNAS, 1992, 89(9), 3686-3690.
|In vitro||DMSO||100 mg/mL warmed (83.15 mM)|
|Ethanol||100 mg/mL warmed (83.15 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
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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|
|NCT03865888||Completed||Drug: Cyclosporins|Drug: Tacrolimus||Dry Eye|Sjogren Syndrome||Pavly Moawd|Cairo University||October 30 2018||Phase 3|
|NCT01762657||Withdrawn||Drug: Oral Cyclosporine and Oral Lansoprazole|Drug: Placebos||Type 1 Diabetes||Perle Bioscience Inc.||September 2014||Phase 3|
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Frequently Asked Questions
What is the difference between S2286 (cyclosporin A) and S1514 (cyclosporin)?
Cyclosporine is a mixture of Cyclosporine A, derivatives of Cyclosporine A, salts of Cyclosporine A. Cyclosporine A is an especially useful Cyclosporine component.