Cyclosporin A
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Cyclosporin A(环孢素A)是一种选择性的亲环素(cyclophilin)抑制剂,IC50值为7 nM[1]。
亲环素是异构酶,参与各种与细胞代谢和能量平衡相关的功能。据报道,亲环素在炎症或恶性肿瘤中过表达。
Cyclosporin A是一种有效的亲环素抑制剂,负责MPTP(线粒体通透性转换孔)的开放。在视网膜神经节细胞中,cyclosporin A对亲环素D的表达具有高选择性,延长细胞存活[2]。在人早期妊娠滋养细胞中,cyclosporin A通过抑制Ca2+/钙调磷酸酶/NFAT信号,从而促进细胞生长和侵袭[3]。Cyclosporin A通过上调Fas/FasL和caspase活性,从而促进T细胞凋亡[4]。在人T细胞中,cyclosporin A通过抑制钙调磷酸酶和NFATc(负责T细胞的功能),从而抑制T细胞活化[1]。据报道,cyclosporin A通过干扰NTCP受体,从而抑制乙型和丙型肝炎病毒的进入[5]。在CRC细胞系(CACO-2、HT-29、HCT-116和LOVO)中,cyclosporin A也可通过非钙调磷酸酶途径影响细胞生长,同时钙调磷酸酶途径也被破坏[6]。
在视网膜缺血的C57BL/6小鼠模型中,cyclosporin A显著阻止亲环素D的上调,改善神经细胞的死亡[2]。
参考文献:
[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.
- 1. Nan Jia, Guo Li, et al. "Staphylococcal superantigen-like protein 10induces necroptosis through TNFR1 activation ofRIPK3-dependent signal pathways." Commun Biol. 2022 Aug 12;5(1):813. PMID: 35962126
- 2. Pengli Liu, Yilong Cui, et al. "Protective effect of mitophagy against aluminum-induced MC3T3-E1 cells dysfunction." Chemosphere. 2021 Nov;282:131086. PMID: 34119729
- 3. Weiwei Qin, Xiyang Tong, et al. "Preservation of mitochondrial homeostasis is responsible for the ameliorative effects of Suhuang antitussive capsule on non-resolving inflammation via inhibition of NF-κB signaling and NLRP3 inflammasome activation." J Ethnopharmacol. 2021 May 10;271:113827. PMID: 33460751
- 4. Zheng ZW, Li J, et al. "Evaluation of in vitro antileishmanial efficacy of cyclosporin A and its non-immunosuppressive derivative, dihydrocyclosporin A." Parasit Vectors. 2020;13(1):94. Published 2020 Feb 21. PMID: 32085719
- 5. 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
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 1202.61 |
Cas No. | 59865-13-3 |
Formula | C62H111N11O12 |
Synonyms | Cyclosporine, Ciclosporin |
Solubility | ≥119.4 mg/mL in DMSO with ultrasonic; insoluble in H2O; ≥101.4 mg/mL in EtOH |
SDF | Download SDF |
Canonical 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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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,24 h |
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(10 μM)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. |
质量控制和MSDS
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