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 7 Publications
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CsA and FTY720 suppress HFD-induced hepatic fat accumulation. Mice were sacrificed at the end of experiment and liver samples were freshly collected and processed. (a) Representative images of liver samples with H&E staining. (b) Representative images of liver samples with Oil Red O staining. Scale bars represent 100 µm.
Pharm Res, 2016, 33(2):395-403. Cyclosporin A purchased from Selleck.
Repression of BSEP gene expression upon treatment with reported BSEP inhibitors in human primary hepatocytes. BSEP mRNA expression was measured using real-time PCR in hepatocytes from at least three donors upon treatment with BSEP inhibitors as described under Materials and Methods. All the data are expressed as mean ?S.D. (n = 3).
Biochim Biophys Acta 2013 1833(3), 652-62. Cyclosporin A purchased from Selleck.
Immunophilins participate in SOCE activation by CN-dependent but also CN-independent signaling pathways. Fura-2 loaded platelets were suspended in HBS, platelets are incubated for 5 min with cyclosporin A (CsA, 50 µM). Once incubation time was over, platelets were stimulated with TG (200 nM) in a calcium free-HBS (EGTA 100 μM was added as indicated the by arrowhead) and 4 min later CaCl2 (300 µM) was added to visualized calcium entry. Changes in fura-2 fluorescence were monitored using the 340/380nm ratio and calibrated in terms of [Ca2+]c . Traces are representative of four to six independent experiments. *,**, *** represents p < 0.05, p < 0.01 and p <0.001, respect control platelets.
Biochim Biophys Acta 2013 1833(3), 652-62. Cyclosporin A purchased from Selleck.
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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 individually and in order:
2% DMSO+corn oil
* 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.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01623167||Recruiting||Aplastic Anemia|Neutropenia|Pancytopenia|Anemia|Thrombocytopenia||National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC)||June 7, 2012||Phase 1|Phase 2|
|NCT02987257||Not yet recruiting||Stevens-Johnson Syndrome|Toxic Epidermal Necrolyses||Ottawa Hospital Research Institute|Canadian Dermatology Foundation|Vanderbilt University|Brooke Army Medical Center||May 2017||Phase 3|
|NCT02887807||Not yet recruiting||Shockable Out of Hospital Cardiac Arrest||Hospices Civils de Lyon||January 2017||Phase 3|
|NCT02876250||Not yet recruiting||Lung Transplantation||Hospices Civils de Lyon||January 2017||Phase 3|
|NCT01962636||Not yet recruiting||Acute Myeloid Leukemia (AML)|Acute Lymphocytic Leukemia (ALL)|Chronic Myelogenous Leukemia|Plasma Cell Leukemia|Myelofibrosis|Myelodysplasia|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma|Marginal Zone B-Cell Lymphoma|Follicular Lymphoma|Lymphoplasmacytic Lymphoma|Mantle-Cell Lymphoma|Prolymphocytic Leukemia|Diffuse Large B Cell Lymphoma|Lymphoblastic Lymphoma|Burkitts Lymphoma|Non-Hodgkin Lymphoma|Multiple Myeloma||Masonic Cancer Center, University of Minnesota||December 2016||--|
|NCT02907554||Not yet recruiting||Brain Death|Kidney Transplantation||University Hospital, Clermont-Ferrand|University Hospital, Estaing|Centre Hospitalier Universitaire de Nice|Groupe Hospitalier Pitie-Salpetriere|Centre Hospitalier Universitaire de Nīmes|University Hospital, Montpellier|Hôtel Dieu (Nantes)|Poitiers University Hospital|University Hospital, Toulouse|Hôpital de la Timone||September 2016||Phase 4|
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.