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环孢菌素A /Cyclosporin A {[allProObj[0].p_purity_real_show]}

货号:A473793 同义名: 环孢素;环孢菌素 / Cyclosporine A;Ciclosporin A

Cyclosporin A是一种免疫抑制剂,能与环孢素结合后抑制钙调神经磷酸酶,IC50为7 nM。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Cyclosporin A 化学结构 CAS号:59865-13-3
Cyclosporin A 化学结构
CAS号:59865-13-3
Cyclosporin A 3D分子结构
CAS号:59865-13-3
Cyclosporin A 化学结构 CAS号:59865-13-3
Cyclosporin A 3D分子结构 CAS号:59865-13-3
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Cyclosporin A 纯度/质量文件 产品仅供科研

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Cyclosporin A 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.

Cyclosporin A 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
guinea pig ventricular myocytes Function assay Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes, IC50=2 μM 22761000

Cyclosporin A 动物研究

Animal study 尿毒症[5]
动物:C57BL/6J ,6-8周龄。
给药:30 mg/kg/天,皮下注射,持续16周。

Cyclosporin A 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.

[5]Nguyen LT, Saad S, Shi Y, Wang R, Chou ASY, Gill A, Yao Y, Jarolimek W, Pollock CA. Lysyl oxidase inhibitors attenuate cyclosporin A-induced nephropathy in mouse. Sci Rep. 2021 Jun 14;11(1):12437.

Cyclosporin A 实验方案

计算器
存储液制备 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

Cyclosporin A 技术信息

CAS号59865-13-3
分子式C62H111N11O12
分子量 1202.61
别名 环孢素;环孢菌素;环胞霉素A ;Cyclosporine A;Ciclosporin A;cyclosporin;Ciclosporin;Cyclosporine;NSC 290193;CsA
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

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

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