Cyclosporin A

製品コードS2286 バッチS228610

印刷

化学情報

Chemical Structure 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
化学式

C62H111N11O12
分子量 1202.61 CAS No. 59865-13-3
Solubility (25°C)* 体外 DMSO 100 mg/mL (83.15 mM)
Ethanol 100 mg/mL (83.15 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
2%DMSO 40%PEG300 5%Tween80 53%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.500mg/ml (2.08mM) Taking the 1 mL working solution as an example, add 20 μL of 125 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.Cyclosporin A (NSC 290193) can be used to induce animal models of Chronic Rejection of Liver Transplantation.
in vitro

Cyclosporin A binds to the cyclophilin (immunophilin) in T cells[1] , forms a Cyclophilin-this compound complex which the binds to and inhibits calcineurin. [2] This chemical inhibits calcineurin with IC50 of 7 nM[3], then blocks the nuclear translocation of NF-AT. [4] It 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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
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.
動物実験 動物モデル Rat
投薬量 45 mg/kg
投与方法 orally

参考

  • https://pubmed.ncbi.nlm.nih.gov/6238408/
  • https://pubmed.ncbi.nlm.nih.gov/1715244/
  • https://pubmed.ncbi.nlm.nih.gov/1373887/
  • https://pubmed.ncbi.nlm.nih.gov/1715516/
  • https://pubmed.ncbi.nlm.nih.gov/8567677/
  • https://pubmed.ncbi.nlm.nih.gov/328380/
  • https://pubmed.ncbi.nlm.nih.gov/7520105/
  • https://link.springer.com/chapter/10.1007/978-94-011-0679-5_12
  • https://pubmed.ncbi.nlm.nih.gov/27725720/

カスタマーフィードバック

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]

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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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