受注:045-509-1970 |
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Synonyms | Cyclosporine A, Cyclosporine, Ciclosporin, CsA,NSC 290193 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C62H111N11O12 |
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分子量 | 1202.61 | CAS No. | 59865-13-3 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL warmed with 50ºC water bath (83.15 mM) | |
Ethanol | 100 mg/mL warmed with 50ºC water bath (83.15 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * 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. |
製品説明 | Cyclosporin A, a non-polar cyclic oligopeptide, is an immunosuppressive agent that binds to cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay. Cyclosporin A is generally given following transplant surgery to prevent rejection and has been used to test its toxic effect on a perfused 3D proximal tubule model. |
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in vitro | Cyclosporin A binds to the cyclophilin (immunophilin) in T cells[1] , forms a Cyclophilin-Cyclosporin A complex which the binds to and inhibits calcineurin. [2] Cyclosporin A inhibits calcineurin with IC50 of 7 nM[3], then blocks the nuclear translocation of NF-AT. [4] Cyclosporin A also affects mitochondria by preventing the MTP (mitochondrial permeability transition pore) from opening with an IC50 of 39 nM. [5] |
in vivo | Cyclosporin A is an immunosuppressive agent that is effective following either parenteral or oral administration in mice, rat and guinea pigs. [6], is clinically used in organ transplantation to prevent rejection. [7] |
キナーゼアッセイ | Phosphatase Assay | |
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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. | ||
細胞アッセイ | 細胞株 | Jurkat cells (clone J77) |
濃度 | ~100 nM | |
反応時間 | 1 hr | |
実験の流れ | 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. |
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動物実験 | 動物モデル | Rat |
投薬量 | 45 mg/kg | |
投与方法 | orally |
Data from [Biochim Biophys Acta, 2013, 1833(3), 652-62]
Data from [Biochim Biophys Acta, 2013, 1833(3), 652-62]
Data from [Data independently produced by , , Pharm Res, 2016, 33(2):395-403]
Select EZH2 inhibitors enhance viral mimicry effects of DNMT inhibition through a mechanism involving NFAT:AP-1 signaling [ Sci Adv, 2024, 10(13):eadk4423] | PubMed: 38536911 |
The cGAS-STING pathway-dependent sensing of mitochondrial DNA mediates ocular surface inflammation [ Signal Transduct Target Ther, 2023, 8(1):371] | PubMed: 37735446 |
The cGAS-STING pathway-dependent sensing of mitochondrial DNA mediates ocular surface inflammation [ Signal Transduct Target Ther, 2023, 8(1):371] | PubMed: 37735446 |
Three-dimensional nanofibrous sponges with aligned architecture and controlled hierarchy regulate neural stem cell fate for spinal cord regeneration [ Theranostics, 2023, 10.7150/thno.87288] | PubMed: 37771775 |
VMP1 affects endoplasmic reticulum stress sensitivity via differential modulation of the three unfolded protein response arms [ Cell Rep, 2023, 42(3):112209] | PubMed: 36870060 |
A novel implant surface modification mode of Fe3O4-containing TiO2 nanorods with sinusoidal electromagnetic field for osteoblastogenesis and angiogenesis [ Mater Today Bio, 2023, 19:100590] | PubMed: 36910272 |
IP3R-dependent mitochondrial dysfunction mediates C5b-9-induced ferroptosis in trichloroethylene-caused immune kidney injury [ Front Immunol, 2023, 14:1106693] | PubMed: 37383224 |
IPSC-Derived Sensory Neurons Directing Fate Commitment of Human BMSC-Derived Schwann Cells: Applications in Traumatic Neural Injuries [ Cells, 2023, 12(11)1479] | PubMed: 37296600 |
Multiparametric Profiling of Neutrophil Function via a High-Throughput Flow Cytometry-Based Assay [ Cells, 2023, 12(5)743] | PubMed: 36899878 |
Epicardial Adipose Tissue-Derived Leptin Promotes Myocardial Injury in Metabolic Syndrome Rats Through PKC/NADPH Oxidase/ROS Pathway [ J Am Heart Assoc, 2023, 12(15):e029415] | PubMed: 37489731 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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