货号:A473793 同义名: 环孢素;环孢菌素 / Cyclosporine A;Ciclosporin A
Cyclosporine A is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 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+ |
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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. |
作用机制 | Cyclosporin A is a calcineurin inhibitor that exerts its immunosuppressive effects via the formation of cyclosporin A-cyclophilin complex. |
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 | ||
Dose | Mice: 5 mg/kg - 15 mg/kg[5] (i.p.) Rat: 10 mg/kg[6] (s.c.) |
Administration | i.p., s.c. |
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 |
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 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
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 |