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 非極性環状オリゴペプチドであるCyclosporin Aは、シクロフィリンに結合し、無細胞アッセイにおいて7 nMのIC50でCalcineurinを阻害する免疫抑制剤です。Cyclosporin Aは通常、移植手術後に拒絶反応を防ぐために投与され、灌流3D近位尿細管モデルに対する毒性効果をテストするために使用されています。Cyclosporin A (NSC 290193) は、肝移植慢性拒絶反応の動物モデルを誘導するために使用できます。
in vitro

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

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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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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