For research use only.
Catalog No.S2286 Synonyms: Cyclosporine A
CAS No. 59865-13-3
Cyclosporin A (Cyclosporine 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.
Selleck's Cyclosporin A has been cited by 36 publications
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|Description||Cyclosporin A (Cyclosporine 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.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04023760||Completed||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|
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
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.