Cyclosporin A

製品コードS2286 バッチS228609

化学情報

	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 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.

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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ	Phosphatase Assay
キナーゼアッセイ	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

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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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