Tamanho : 50mg
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Synonyms: Cyclosporine A, Cyclosporine, Ciclosporin
| Description | Cyclosporin A is a natural product and an active fungal metabolite, classified as a cyclic polypeptide immunosuppressant. It binds to cyclophilin and inhibits the activity of calcineurin (IC₅₀ = 7 nM) as well as CD11a/CD18 adhesion molecules. It is commonly used to induce uremia models. |
| Targets & IC50 | U-87MG cells viability:10 μM, CYP450 (Rat):0.4 μM (Ks), Calcineurin phosphatase:7 nM |
| In vitro | METHODS: Glioma cell C6 was treated with Cyclosporin A (10 μM) under hypoxic conditions for 4 h. The expression levels of target proteins were measured by Western Blot. RESULTS: 4 h hypoxia induced a large accumulation of endogenous HIF-1α protein, and Cyclosporin A prevented most of the hypoxia-induced HIF-1α stabilization. [1] METHODS: Human colon cancer cells CACO-2 were treated with Cyclosporin A (2 μM) for 24-72 h. The cell cycle was detected by Flow Cytometry. RESULTS: Accumulation of cells was detected in the G0/G1 phase after treatment with Cyclosporin A. The RESULTS were summarized in the following table. [2] |
| In vivo | METHODS: To assay activity against muscle disease in vivo, Cyclosporin A (5 mg/kg in olive oil) was injected intraperitoneally into myopathic Col6a1-/- mice twice daily for ten days. RESULTS: Cyclosporin A affected satellite cell activity and triggered regenerative fiber formation in Col6a1-/- mice. [3] METHODS: To detect the effects on ischemia-reperfusion injury (IRI), Cyclosporin A (3 mg/kg, 1 h or 10 min before ischemia; 10 mg/kg, 10 min before ischemia) was intraperitoneally injected into ischemia-reperfused C57BL/6J mice. RESULTS: Mortality and renal function were significantly higher in the Cyclosporin A 10 mg/kg-10 min and Cyclosporin A 3 mg/kg-1 h groups than in the Cyclosporin A 3 mg/kg-10 min group. [4] |
| Synonyms | Cyclosporine A, Cyclosporine, Ciclosporin |
| Disease Modeling Protocol | Chronic kidney disease model
*Precautions： The mice were euthanized by cardiac puncture during deep anesthesia. *References：Nguyen LT,et,al. Lysyl oxidase inhibitors attenuate cyclosporin A-induced nephropathy in mouse. Sci Rep. 2021 Jun 14;11(1):12437. |
| Kinase Assay | 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. |
| Cell Research | Immunosuppressive agents are dissolved in ethanol at concentrations 1000-fold more than the concentration desired for cell treatments. Cells (106) are suspended in 1 ml of complete medium in microcentrifuge tubes; 1 μl of ethanol or of the ethanolic solution of Cyclosporin A is added, and the cells are incubated at 37°C for 1 hr. Cells are washed twice with 1 ml of PBS on ice and lysed in 50μl of hypotonic buffer containing 50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM dithiothreitol; and 50 μg of phenylmethylsulfonyl fluoride, 50 μg of soybean trypsin inhibitor, 5 μg of leupeptin, and 5 μg of aprotinin per ml. Lysates are subjected to three cycles of freezing in liquid nitrogen followed by thawing at 30°C and then are centrifuged at 4°C for 10 min at 12,000×g.(Only for Reference) |
| Molecular Weight | 1202.61 |
| Formula | C62H111N11O12 |
| Cas No. | 59865-13-3 |
| Smiles | [C@H]([C@@H](C/C=C/C)C)(O)[C@@]1(N(C)C(=O)[C@H]([C@@H](C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H]([C@H](C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C(=O)[C@H](CC)NC1=O)04 |
| Relative Density. | 0.9913 g/cm3 (Estimated) |
| Storage | Keep away from moisture,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 255 mg/mL (212.04 mM), Sonication is recommended.  Ethanol: 60.1 mg/mL (49.97 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 12.03 mg/mL (10 mM), Suspension. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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