Cyclosporin A (Synonyms: 环bao素; Cyclosporine A; Ciclosporin A; CsA)
Cyclosporin A (Cyclosporine A) 是一种免疫抑制剂，能与亲环素结合，抑制 calcineurin 活性的IC50 值为 7 nM。Cyclosporin A 也抑制 CD11a/CD18 粘附分子。
生物活性
Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM[3]. Cyclosporin A also inhibits CD11a/CD18 adhesion[8].
IC50 & Target
IC50: 7 nM (calcineurin)
体外研究(In Vitro)
Cyclosporin A is able to bind with the cyclophilin in T cells[1]. Cyclosporin A works by forming a Cyclophilin-Cyclosporin A complex to inhibit calcineurin[2]. Cyclosporin A inhibits calcineurin in stimulated cells with an IC50 value of 7 nM[3]. Cyclosporin A suppresses the nuclear translocation of NF-AT[4]. Cyclosporin A shows an effect on mitochondria via preventing the MTP from opening with an IC50 of 39 nM[5].
体内研究(In Vivo)
Cyclosporin A has immunosuppressive activity, and is active via parenteral and p.o. administration in mice, rat and guinea pigs[6]. Cyclosporin A can be used in organ transplantation to prevent rejection[7].
分子量：1202.61
性状：Solid
Formula：C62H111N11O12
CAS 号：59865-13-3
中文名称：huan孢霉素A；环孢suA；环bao多肽A；环孢灵；赛斯平；环bao素
来源：the fungus Beauveria nivea.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
DMSO : 62.5 mg/mL (51.97 mM; Need ultrasonic)
Ethanol : 50 mg/mL (41.58 mM; Need ultrasonic)
| 浓度溶剂体积质量 | 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 | 1.6630 mL |
| 10 mM | 0.0832 mL | 0.4158 mL | 0.8315 mL |
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, 6 months; -20°C, 1 month (protect from light)。-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。
以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制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
- 1.
请依序添加每种溶剂： corn oil
Solubility: 20 mg/mL (16.63 mM); Clear solution; Need ultrasonic
- 2.
请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: 2.62 mg/mL (2.18 mM); Suspended solution; Need ultrasonic
- 3.
请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (1.73 mM); Suspended solution; Need ultrasonic
- 4.
请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (1.73 mM); Suspended solution; Need ultrasonic
- 5.
请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (1.73 mM); Clear solution
参考文献
[1]. Handschumacher RE, et al. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984 Nov 2;226(4674):544-7. [Content Brief]
[2]. Liu J, et al. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15. [Content Brief]
[3]. Fruman DA, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc Natl Acad Sci U S A. 1992 May 1;89(9):3686-90. [Content Brief]
[4]. Flanagan WM, et al. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A. Nature. 1991 Aug 29;352(6338):803-7. [Content Brief]
[5]. Nicolli A, 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 Jan 26;271(4):2185-92. [Content Brief]
[6]. Borel JF, et al. Effects of the new anti-lymphocytic peptide cyclosporin A in animals. Immunology. 1977 Jun;32(6):1017-25. [Content Brief]
[7]. Williams, R, et al. Randomised trial comparing FK506 and cyclosporin in prevention of liver allograft rejection. European FK506 Multicentre Liver Study Group. Lancet, 1994, 344(8920), 423-428. [Content Brief]
[8]. Dalmarco EM, et al. Cyclosporin A inhibits CD11a/CD18 adhesion molecules due to inhibition of TNFalpha and IL-1 beta levels in the mouse model of pleurisy induced by carrageenan. Cell Adh Migr. 2008 Oct-Dec;2(4):231-5. [Content Brief]
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