Cyclosporine
(Synonyms: 环孢素A,CsA; Cyclosporine A; Ciclosporin A) 目录号 : GC11328
An immunosuppressant
Cas No.:59865-13-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
|
Cell lines |
EMG7 mouse ES cells, systematically induced from mesodermal precursor, Flk1 (also designated as vascular endothelial growth factor receptor-2 (VEGFR2))-expressing cells. |
|
Preparation method |
The solubility of this compound in DMSO is >53mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
1–3μg/mL |
|
Applications |
Addition of cyclosporine (1–3 μg/mL) to Flk1+ cells showed a striking effect to increase beating cells at Flk-d6 and induced approximately 13 times increase in cardiac troponin-T (cTnT)-positive cardiomyocyte appearance than control. These results indicated that functional cardiomyocytes were successfully induced and expanded by cyclosporine treatment. Addition of cyclosporine to Flk1+ cells specifically increased FCV (Flk1+/CXCR4+/vascular) population to approximately 10–20 times more than control. The maximum percentage of FCV cells within total Flk1+ cell-derived cells was increased up to 40% by cyclosporine. The yield of purified FCV progenitor cells was increased approximately 22 times by cyclosporine treatment. These results indicate that cyclosporine-expanded FCV cells retained their high cardiogenic potentials. Taken together, cyclosporine showed a novel effect specifically acting on mesoderm cells to drastically increase cardiac progenitors as well as cardiomyocytes by 10–20 times. Expanded FCV cardiac progenitors showed differentiation potentials to cardiomyocytes in vivo after cell transplantation to rat myocardial infarction model. |
| Animal experiment [2]: | |
|
Animal models |
mice of 7-12 weeks (the inbred strains C3H,C57BL/6 and BALB/c);outbred guinea-pigs of both sexes |
|
Dosage form |
Male mice (SIM and C3H) , gavage 250 mg/kg/day on 5 consecutive days; Guinea-pigs i.p. 20-50mg/kg/day on 4 consecutive days. |
|
Application |
Doses of cyclosporin on consecutive days strongly depressed direct PFC (plaque-forming cells) in rats in a dose-dependent manner. cyclosporin markedly depresses both direct and indirect PFC in mice on day 4.In another similar skin contact sensitivity model using DNCB (1-chlor-2,4-dinitrobenzene) in guinea pigs, i.p. Treatment on days 0-4 with either 20 or 50 mg/kg/day of cyclosporin completely suppressed the skin reaction on day 10 since no redness nor swelling were observed. The inhibition caused by cyclosporin seems to affect mainly the effector cells and was achieved at well-tolerated doses. Cyclosporin has, in addition, been shown to depress not only the primary response, but also the secondary response of both IgM and IgG2a PFC, oxazolone hypersensitivity. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Peishi Yan , Atsushi Nagasawa , Hideki Uosaki ., et al.Cyclosporin-A potently induces highly cardiogenic progenitors from embryonic stem cells. BiochemsBiophys.Res.Commun. 379 (2009) 115–120. [2]. Borel JF, Feurer C, Magnée C., et al. Effects of the new anti-lymphocytic peptide cyclosporin A in animals. Immunology. 1977 Jun;32(6):1017-25. |
|
Cyclosporine (cyclosporin A), a immunosuppressive agent, inhibits phosphatase activity of calcineurin with IC50 value of 5 nM [1].
The immunosuppressive agent cyclosporin A (CsA) binds to soluble cytosolic proteins named cyclophilins, and the complex of cyclophilin–CsA blocks calcineurin, which inhibits stimulation of the NFAT-induced genes which are required for the activation of T cells.
As a widely used immunosuppressive agent, cyclosporin A has been reported to be effective against HCV infection. The anti-viral effects of CsA has been investigated by an HCV replicon system. Huh7/Rep-Feo cells treated with CsA with an IC50 value of about 0.5 μg/ml resulted in suppression of the replication of the HCV replicon in a dose-dependent manner. There were no changes in the rate of cell growth or viability, revealing that the specific effect of CsA against HCV is not due to cytotoxicity. CsA inhibits HCV replication in vitro specifically at clinical concentrations [2].
Transplantation of CSA-expanded FCV cells to chronic myocardial infarction was performed in the model of rat. Transplanted FCV cells were successfully differentiated into cardiomyocytes and integrated in the infarct heart to form GFP+/cTnT+ donor cell-derived cardiomyocyte bundle in the scar tissue in 2 weeks after the injection. The result show that CSA-expanded FCV cells can show highly cardiogenic potentials also in vivo after cell transplantation [3].
环孢霉素（环孢霉素A）是一种免疫抑制剂，抑制钙调神经酶的磷酸酶活性，IC50值为5 nM [1]。 免疫抑制剂环孢霉素A（CsA）结合可溶性细胞质蛋白环状蛋白，环状蛋白-CsA复合物阻碍钙调神经酶，从而抑制了NFAT诱导基因的激活，这些基因对于T细胞的激活是必需的。 作为一种广泛使用的免疫抑制剂，环孢霉素A已被报道对丙型肝炎病毒（HCV）感染有效。 CsA的抗病毒效应已通过HCV复制子系统进行了研究。用约0.5 μg/ml的CsA处理Huh7/Rep-Feo细胞，可以在剂量依赖性下抑制HCV复制子的复制。细胞生长或活力没有变化，表明CsA对HCV的特定作用不是由于细胞毒性引起的。CsA以临床浓度特异性地抑制HCV的复制 [2]。 在大鼠慢性心肌梗死模型中，将经CSA扩增的FCV细胞移植到心肌梗死部位。移植的FCV细胞成功分化为心肌细胞，并在注射后2周内集成到梗死心脏中形成GFP+/cTnT+供体细胞衍生的心肌细胞束。结果表明，CSA扩增的FCV细胞也可以在体内展示高度的心脏形成潜力 [3]。
References:
[1]. Fruman DA , Klee CB, Bierer BE, et al. Calcineurin Phosphatase-Activity In Lymphocytes-T Is Inhibited By Fk-506 And Cyclosporine-A. Proceedings Of The National Academy Of Sciences Of The United States Of America. 1992, 89(9): 3686-3690.
[2]. Nakagawa M, Sakamoto N, Enomoto N, et al. Specific inhibition of hepatitis C virus replication by cyclosporin A. Biochemical And Biophysical Research Communications. 2004, 313(1): 42-47.
[3]. Yan P, Nagasawa A, Uosaki H, et al. Cyclosporin-A potently induces highly cardiogenic progenitors from embryonic stem cells. Biochemical And Biophysical Research Communications. 2009, 379(1): 115-120.
| Cas No. | 59865-13-3 | SDF | |
| 别名 | 环孢素A,CsA; Cyclosporine A; Ciclosporin A | ||
| 化学名 | 30-ethyl-33-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone | ||
| 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 | ||
| 分子式 | C62H111N11O12 | 分子量 | 1202.61 |
| 溶解度 | >53mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 0.8315 mL | 4.1576 mL | 8.3152 mL |
| 5 mM | 0.1663 mL | 0.8315 mL | 1.663 mL |
| 10 mM | 0.0832 mL | 0.4158 mL | 0.8315 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。