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Cyclosporin A

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Catalog No.
B1922
免疫抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
100mg
¥ 500.00
现货
200mg
¥ 700.00
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500mg
¥ 1,000.00
现货

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Background

Cyclosporin A is a selective cyclophilin inhibitor with IC50 value of 7 nM [1].

Cyclophilins are isomerase enzymes and involve in a variety of functions related to cell metabolism and energy homeostasis. It has been reported that the over expression of cyclophilins were observed in inflammation or malignancy.

Cyclosporin A is a potent cyclophilin inhibitor which is responsible for the opening of the MPTP (mitochondrial permeability transition pore). When tested with retinal ganglion cells, Cyclosporin A showed a high selectivity for the expression of cyclophilin D and prolonged the cells survival [2]. In human First-Trimester Trophoblast Cells, Cyclosporin A treatment promoted cells growth and invasiveness by inhibiting Ca2+/Calcineurin/NFAT signal [3]. Cyclosporin A treatment promoted the apoptosis of T-cell by upregulating Fas/FasL and caspase activities [4]. Treated human T cells with Cyclosporin A suppressed T cell activation by inhibiting calcineurin and NFATc which are responsible for T cell function [1].

In retinal ischemia C57BL/6 mouse model, Cyclosporin A treatment significantly prevented the up regulation of cyclophilin D and ameliorated the death of neuronal cells in vivo [2].

Cyclosporin A has also been reported to inhibit the entry of hepatitis B and C virus through interfering NTCP reportor [5]. In CRC cell lines (CACO-2, HT-29, HCT-116 and LOVO), Cyclosporin A treatment also could impair cell growth via without calcineurin pathway while the mechanism was still undermined [6].

References:
[1].  Minguillon, J., et al., Concentrations of cyclosporin A and FK506 that inhibit IL-2 induction in human T cells do not affect TGF-beta1 biosynthesis, whereas higher doses of cyclosporin A trigger apoptosis and release of preformed TGF-beta1. J Leukoc Biol, 2005. 77(5): p. 748-58.
[2].  Kim, S.Y., et al., Inhibition of cyclophilin D by cyclosporin A promotes retinal ganglion cell survival by preventing mitochondrial alteration in ischemic injury. Cell Death Dis, 2014. 5: p. e1105.
[3].  Du, M.R., et al., Cyclosporin A promotes growth and invasiveness in vitro of human first-trimester trophoblast cells via MAPK3/MAPK1-mediated AP1 and Ca2+/calcineurin/NFAT signaling pathways. Biol Reprod, 2008. 78(6): p. 1102-10.
[4].  Gao, J., et al., Mitochondrial permeability transition pore in inflammatory apoptosis of human conjunctival epithelial cells and T cells: effect of cyclosporin A. Invest Ophthalmol Vis Sci, 2013. 54(7): p. 4717-33.
[5].  Nkongolo, S., et al., Cyclosporin A inhibits hepatitis B and hepatitis D virus entry by cyclophilin-independent interference with the NTCP receptor. J Hepatol, 2014. 60(4): p. 723-31.
[6].  Werneck, M.B., et al., Cyclosporin A inhibits colon cancer cell growth independently of the calcineurin pathway. Cell Cycle, 2012. 11(21): p. 3997-4008.

文献引用

1. Yang YL, Li J, et al. "Ginsenoside Rg5 increases cardiomyocyte resistance to ischemic injury through regulation of mitochondrial hexokinase-II and dynamin-related protein 1." Cell Death Dis. 2017 Feb 23;8(2):e2625. PMID:28230856

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt1202.61
Cas No.59865-13-3
FormulaC62H111N11O12
SynonymsCyclosporine, Ciclosporin
Solubility≥60.15mg/mL in DMSO
SDFDownload SDF
Canonical SMILESCCC1C(=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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

Jurkat T细胞和A549肺癌细胞

溶解方法

该化合物在DMSO中的溶解度大于60.2 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

1 μM,24h

应用

在初次TCR刺激期间用CsA预处理新鲜T细胞,降低了TGF-β1的产生。较高浓度的CsA(10μM)通过诱导细胞凋亡促进预先形成的TGF-β1的释放。

动物实验 [2]:

动物模型

雌性视网膜缺血C57BL/6小鼠模型

给药剂量

腹腔注射,5 mg/kg每天

应用

CsA显著促进缺血性视网膜的RGC存活。CsA治疗12小时后明显减少缺血性视网膜中的GFAP和CypD蛋白表达。CsA减少缺血性视网膜内层的CypD免疫反应性。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Minguillón J, Morancho B, Kim S J, et al. Concentrations of cyclosporin A and FK506 that inhibit IL-2 induction in human T cells do not affect TGF-β1 biosynthesis, whereas higher doses of cyclosporin A trigger apoptosis and release of preformed TGF-β1[J]. Journal of leukocyte biology, 2005, 77(5): 748-758.

[2]. Kim S Y, Shim M S, Kim K Y, et al. Inhibition of cyclophilin D by cyclosporin A promotes retinal ganglion cell survival by preventing mitochondrial alteration in ischemic injury[J]. Cell death & disease, 2014, 5(3): e1105.

质量控制

化学结构

Cyclosporin A

相关生物数据

Cyclosporin A