Cyclosporin A

別名：Cyclosporine A, Cyclosporine, Ciclosporin, CsA,NSC 290193

製品コード：S2286 純度：99.98%

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.

CAS No. 59865-13-3

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
50mg	JPY 22000	国内在庫あり
200mg	JPY 44500	国内在庫あり
1g	JPY 118500	国内在庫あり

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製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

Cyclosporin Aと併用されることが多い化合物

Diquafosol Tetrasodium

Cyclosporin A and Diquafosol Tetrasodium combination therapy significantly improves the objective signs and symptoms of dry eyes.

Eom Y, et al. J Ocul Pharmacol Ther. 2022 Dec;38(10):682-694.

Rapamycin

Cyclosporin A and Rapamycin exhibits complete inhibition of experimental autoimmune uveoretinitis (EAU) in rats.

Martin DF, et al. J Immunol. 1995 Jan 15;154(2):922-7.

Cyclosporin A関連製品

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関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

Antineoplastic and Immunosuppressive Antibiotics阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
human K562/R7 cells	Function assay	1 μM	72 h	Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay, IC50=0.7 μM	25634041
MDCK2	Function assay	10 uM	40 mins	Inhibition of human wild type Pgp expressed in MDCK2 cells assessed as calcein-AM accumulation at 10 uM after 40 mins.	17964170
C2C12	Function assay	0.1 ug/ml	3 days	Inhibition of hexose-6-phosphate dehydrogenase-induced cell differentiation in mouse C2C12 cells assessed as myosin heavy chain fluorescence at 0.1 ug/ml for 3 days.	20081855
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

calcineurin ^[1]
(Cell-free assay)

7 nM

In Vitro
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]
Kinase Assay	Phosphatase Assay
Kinase 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.
細胞実験	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.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	Phospho-AKT1 / AKT1 / PTEN / Phospho-BAD / BAD / Procaspase-3 Cyp-D / AIF / β-actin IL-8 / MCP-1 Actin / Smac β-actin / FIPV-N		12644839
	Growth inhibition assay	NPC death		20181586
	IHC	Th22 / Th17 / Th1 / M1 / Th2 Tregs / Bregs / pDCs / M2 Ki 67 / Fas-FasL IFN-γ / TNF-α WT-PCLS / FXRKO-PCLS		30916387
	Immunofluorescence	Human gingival fibroblast cells Human gingival fibroblast cells Calcein Rhod-Dex / Calcein cadherin-9 / vimentin		27857765

In Vivo
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]
動物実験	動物モデル	Rat
	投与量	45 mg/kg
	投与経路	orally

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06366685	Not yet recruiting	Esophageal Cancer\|Exercise Training\|Psychotherapy\|Rehabilitation	Mengmeng Yuan\|Anhui Medical University	May 1 2024	Not Applicable
NCT06320561	Not yet recruiting	Stroke	Vrije Universiteit Brussel\|University Ghent\|Research Foundation Flanders	May 2024	--
NCT05702931	Not yet recruiting	Hyperglycemia\|Renal Transplant Complication Primary Non-Function\|Diabetes	Rigshospitalet Denmark\|Aarhus University Hospital\|Odense University Hospital	April 1 2024	Phase 4
NCT06052761	Recruiting	Child in Hospital	Adiyaman University	February 10 2024	Not Applicable

参考
[1] Handschumacher RE, et al. Science, 1984, 226(4674), 544-547. [2] Liu J, et al. Cell, 1991, 66(4), 807-815. [3] Fruman DA, et al. PNAS, 1992, 89(9), 3686-3690. [4] Flanagan WM, et al. Nature, 1991, 352(6338), 803-807. [5] Nicolli A, et al. J Biol Chem, 1996, 271(4), 2185-2192. [6] Borel JF, et al. Immunology, 1977, 32(6), 1017-1025. [7] Williams, R, et al. Lancet, 1994, 344(8920), 423-428. [8] https://link.springer.com/chapter/10.1007/978-94-011-0679-5_12 [9] Homan KA, et al. Sci Rep. 2016 Oct 11;6:34845. + 展開

参考

+ 展開

化学情報

分子量	1202.61	化学式	C₆₂H₁₁₁N₁₁O₁₂
CAS No.	59865-13-3	SDF	Download Cyclosporin A SDFをダウンロードする
Smiles	CCC1C(=O)N(CC(=O)N(C(C(=O)NC(C(=O)N(C(C(=O)NC(C(=O)NC(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N1)C(C(C)CC=CC)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (83.15 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 100 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

Clear solution

2%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 53%ddH2O

2.5mg/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.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問1:
What is the difference between S2286 (cyclosporin A) and S1514 (cyclosporin)?

回答
Cyclosporine is a mixture of Cyclosporine A, derivatives of Cyclosporine A, salts of Cyclosporine A. Cyclosporine A is an especially useful Cyclosporine component.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):