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首页 / 抑制剂/激动剂 / 免疫/炎症 / Cyclophilin / Cyclosporin A/环孢菌素A

Cyclosporin A/环孢菌素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+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Cyclosporin A/环孢菌素A 化学结构 CAS号：59865-13-3
Cyclosporin A/环孢菌素A 化学结构
CAS号：59865-13-3
Cyclosporin A/环孢菌素A 3D分子结构
CAS号：59865-13-3
Cyclosporin A/环孢菌素A 化学结构 CAS号：59865-13-3
Cyclosporin A/环孢菌素A 3D分子结构 CAS号：59865-13-3
规格 价格 会员价 库存 数量
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Cyclosporin A/环孢菌素A 纯度/质量文件 产品仅供科研

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Cyclosporin A/环孢菌素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/环孢菌素A 细胞实验

Cell Line
Concentration Treated Time Description References
HMEC-1 2.5 μM 24 h To evaluate the inhibitory effect of Cyclosporin A on P-gp, the results showed that Cyclosporin A effectively inhibited P-gp function, thereby reversing the resistance of HMECd1 and HMECd2 cells to Dox. J Hematol Oncol. 2013 Jul 9;6:49.
D1 cells 0.000-10.000 μg/ml 4 h Cyclosporin A and FK506 effectively suppressed WGP-induced NFAT-luciferase activity, indicating that Cyclosporin A inhibits NFAT activity in D1 cells by suppressing NFAT nuclear translocation. Nat Commun. 2018 Mar 16;9(1):1102.
HeLa cells 4 µM To test the inhibitory effect of Cyclosporin A on the mitochondrial permeability transition pore (PTP), results showed that CsA could completely inhibit PTP opening. Nat Commun. 2021 Aug 10;12(1):4835.
HAP1 cells 4 µM To test the inhibitory effect of Cyclosporin A on PTP, results showed that CsA could inhibit PTP in wild-type HAP1 cells but not in Δb and ΔOSCP cells. Nat Commun. 2021 Aug 10;12(1):4835.
Activated B blasts 1 µg/ml To generate proliferating B cells and study their role in EBV infection PLoS Biol. 2005 Dec;3(12):e404.
Lymphoblastoid cell lines 2 μg/ml Used for the generation and culture of lymphoblastoid cell lines EBioMedicine. 2021 Sep;71:103572.

Cyclosporin A/环孢菌素A 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Yucatan pigs Delayed type hypersensitivity model Oral 60 mg/kg CsA Twice, at 12 hours before and 3 hours after challenge To evaluate the inhibitory effect of CsA on DTH reaction in pig ears. Results showed that CsA significantly reduced ear redness, inflammatory cell accumulation, and inflammatory mediator release. Toxins (Basel). 2009 Sep;1(1):25-36
Pig Healthy pig heart Intravenous injection 100-120 ng/ml Once daily for 40 days To test the engraftment and differentiation potential of 13R2+ cells in pig hearts, the results showed that 13R2+ cells could survive, engraft, and differentiate into definitive cardiovascular cell types in the pig heart after approximately 6 weeks. Stem Cell Reports. 2016 Jan 12;6(1):95-108
BALB/c mice Neuroblastoma model Ip injection 10 mg/kg For 5 consecutive days To evaluate the effect of cyclosporin A on the toxicity of vincristine, results showed that cyclosporin A significantly increased the toxicity of vincristine. Cancer Res. 2009 Aug 15;69(16):6573-80.
Mice Acute renal allograft rejection model Subcutaneous injection 5 mg/kg Daily for 7 days To study the immunosuppressive effect of Cyclosporin A in an acute renal allograft rejection model, results showed that Cyclosporin A effectively suppressed rejection. Transplantation. 2020 Apr;104(4):744-753

Cyclosporin A/环孢菌素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/环孢菌素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/环孢菌素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/环孢菌素A 技术信息

CAS号59865-13-3
分子式C62H111N11O12
分子量 1202.61
SMILES Code O[C@@H]([C@](C(N[C@H](C(N(CC(N([C@H](C(N[C@@](C(N([C@H]1CC(C)C)C)=O)([H])C(C)C)=O)CC(C)C)C)=O)C)=O)CC)=O)([H])N(C([C@](N(C([C@@H](N(C([C@H](N(C([C@H](NC([C@@H](NC1=O)C)=O)C)=O)C)CC(C)C)=O)C)CC(C)C)=O)C)([H])C(C)C)=O)C)[C@H](C)C/C=C/C
MDL No. MFCD00274558
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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
方案 四
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Cyclosporin A | Cyclosporine A;Ciclosporin A;cyclosporin;Ciclosporin;Cyclosporine;NSC 290193;CsA | 环孢素;环孢菌素;环胞霉素A | Oligopeptide | Calcineurin Inhibitor | Polypeptide | Calcineurin | AmBeed-信号通路专用抑制剂 | Cyclosporin A/环孢菌素A 纯度/质量文件 | Cyclosporin A/环孢菌素A 生物活性 | Cyclosporin A/环孢菌素A 动物研究 | Cyclosporin A/环孢菌素A 参考文献 | Cyclosporin A/环孢菌素A 实验方案 | Cyclosporin A/环孢菌素A 技术信息

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