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Cyclosporin A

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Chemical Structure| 59865-13-3 同义名 : 环孢素;环孢菌素;环胞霉素A ;Cyclosporine A;Ciclosporin A;cyclosporin;Ciclosporin;Cyclosporine;NSC 290193;CsA
CAS号 : 59865-13-3
货号 : A473793
分子式 : C62H111N11O12
纯度 : 97% HPLC
分子量 : 1202.61
MDL号 : MFCD00274558
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(49.89 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 45 mg/mL(37.42 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：

SC 10% DMSO+90% corn oil 5 mg/mL clear

生物活性
描述 Cyclosporin A is an immunosuppressant which binds to its receptor cyclophilin (CyP) by forming drug-dependent complexes to inhibit the activity of calmodulin-dependent phosphatase calcineurin (IC50=7 nM)[1]. Cyclosporin A appears to specifically inhibit the early events of T lymphocyte activation by blocking the transcription of NF-AT, which is essential for early T-cell gene activation[2]. Moreover, it has been demonstrated that Cyclosporin A can inhibit nitric oxide synthesis induced by interleukin-alpha, lipopolysaccharide and NF-κB. Nanomolar concentrations of Cyclosporin A (IC50 = 39 nM) displays an inhibition of the permeability transition pore (MTP) opening of an inner membrane channel in Mammalian mitochondria[3]. Studies in animals indicate that Cyclosporin A can induce apoptosis of rat lymphocytes and mouse B-cell lymphoma cell line WEHI-231. Notably, Cyclosporin A was found to be widely used for treating rejecting of allogenic transplant to prevent the activity of the patient's immune system[4]. It has been studied in transplants of skin, kidney, liver, small intestine, bone marrow and so on.
作用机制 Cyclosporin A is a calcineurin inhibitor that exerts its immunosuppressive effects via the formation of cyclosporin A-cyclophilin complex.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A2780/ADR cells Function assay Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay， IC50=1.41254 μM 17890094
african green monkey Vero cells Function assay 24 h Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay, IC50=8 μM 19451286
CK1 cells Function assay Antiviral activity against HPV-33 infected in CK1 cells assessed as inhibition of viral replication after 7 days, TC50=0.3 μM 18212100
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.83mL

0.17mL

0.08mL

4.16mL

0.83mL

0.42mL

8.32mL

1.66mL

0.83mL
参考文献

[1]Handschumacher RE, Harding MW, et al. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984;226(4674):544-7.

[2]Flanagan WM, Corthesy B, et al. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A. Nature. 1991;352(6338):803-7.

[3]Nicolli A, Basso E, et al. Interactions of cyclophilin with the mitochondrial inner membrane and regulation of the permeability transition pore, and cyclosporin A-sensitive channel. J Biol Chem. 1996;271(4):2185-92.

[4]Emmel EA, Verweij CL, et al. Pillars Article: Cyclosporin A Specifically Inhibits Function of Nuclear Proteins Involved in T Cell Activation. Science. 1989. 246: 1617-1620. J Immunol. 2018;201(11):3149-3152.