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My CartCAS：59865-13-3
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 59865-13-3 |
| Name | Cyclosporin A |
| Molecular Formula | C62H111N11O12 |
| Molecular Weight | 1202.61 |
| Solubility | Soluble in DMSO ≥10mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 200-835-2 |
| MDL | MFCD00274558 |
| SMILES | O[C@@H]([C@](C(N[C@H](C(N(CC(N([C@H](C(N[C@@](C(N([C@H]1CC(C)C)C)=O)([H])C(C)C)=O)CC(C)C)C)=O)C)=O)CC)=O)([H])N(C([C@](N(C([C@@H](N(C([C@H](N(C([C@H](NC([C@@H](NC1=O)C)=O)C)=O)C)CC(C)C)=O)C)CC(C)C)=O)C)([H])C(C)C)=O)C)[C@H](C)C/C=C/C |
| InChIKey | PMATZTZNYRCHOR-CGLBZJNRSA-N |
| InChI | InChI=1S/C62H111N11O12/c1-25-27-28-40(15)52(75)51-56(79)65-43(26-2)58(81)67(18)33-48(74)68(19)44(29-34(3)4)55(78)66-49(38(11)12)61(84)69(20)45(30-35(5)6)54(77)63-41(16)53(76)64-42(17)57(80)70(21)46(31-36(7)8)59(82)71(22)47(32-37(9)10)60(83)72(23)50(39(13)14)62(85)73(51)24/h25,27,34-47,49-52,75H,26,28-33H2,1-24H3,(H,63,77)(H,64,76)(H,65,79)(H,66,78)/b27-25+/t40-,41+,42-,43+,44+,45+,46+,47+,49+,50+,51+,52-/m1/s1 |
| PubChem CID | 5284373 |
| Target Point | Others |
| Passage | Others |
| Background | Cyclosporin A is an immunosuppressant that binds cyclophilin and inhibits the phosphatase activity of calcineurin. |
| Biological Activity | Cyclosporin 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。[1-7] |
| In Vitro | 环孢菌素A能够与T细胞中的亲环蛋白结合[1]。环孢菌素A通过形成亲环蛋白 - 环孢菌素A复合物来抑制神经钙蛋白[2]。环孢菌素A对钙调神经磷酸酶具有抑制作用，IC50为7 nM [3]。环孢菌素A抑制NF-AT的核转位[4]。环孢菌素A通过阻止MTP打开显示对线粒体的影响，IC50为39 nM [5]。 |
| In Vivo | 环孢菌素A具有免疫抑制活性，并且在小鼠，大鼠和豚鼠中通过肠胃外和口服给药具有活性[6]。环孢菌素A可用于器官移植以防止排斥反应[7]。 |
| Cell Experiment | 免疫抑制剂以比细胞处理所需浓度高1000倍的浓度溶解在乙醇中。将细胞(106)悬浮于微量离心管中的1mL完全培养基中;加入1μL乙醇或环孢菌素A的乙醇溶液，并将细胞在37℃下孵育1小时。将细胞在冰上用1mL PBS洗涤两次，并在含有50mM Tris(pH 7.5)的50μL低渗缓冲液中裂解; 0.1mM EGTA; 1 mM EDTA; 0.5mM二硫苏糖醇;每毫升50μg苯甲基磺酰氟，50μg大豆胰蛋白酶抑制剂，5μg亮肽素和5μg抑肽酶。将裂解物在液氮中进行三个循环的冷冻，然后在30℃下解冻，然后在4℃下以12，000×g离心10分钟。 |
| Animal Experiment | 在第0天腹膜内用0 5mL免疫大鼠，小鼠静脉内用0 2mL 10％洗过的绵羊红细胞(SE)悬浮液免疫。为了引起二次反应，在初次免疫后8-11周，用静脉内注射0-2mL的25％洗涤的SE(107个细胞)对小鼠进行加强免疫。对于长期治疗，动物在13周内每天在食物中平均接受45mg/kg环孢菌素A.在杀死前5天对这些大鼠进行免疫。 |
| Kinase Experiment | 与纯化酶的反应混合物含有100 nM钙调神经磷酸酶，100 nM钙调蛋白和5μM32P标记的磷酸肽，在60μL(总体积)的含有20 mM Tris(pH 8)，100 mM NaCl，6 mM MgCl 2，0.5的分析缓冲液中mM二硫苏糖醇，每毫升0.1mg牛血清白蛋白，和0.1mM CaCl 2或5mM EGTA。与细胞裂解物的反应混合物含有20μL未稀释的裂解物，5μM32P标记的磷酸肽和40μL测定缓冲液。反应混合物含有50μM肽412或413和/或500nM冈田酸，磷酸酶1和2A的特异性抑制剂; 500nM冈田酸足以抑制Ca2 +非依赖性磷酸酶，而较高浓度也部分抑制Ca2 +依赖性磷酸酶活性。在30℃下15分钟后，通过加入0.5mL含有5％三氯乙酸的100mM磷酸钾缓冲液(pH7.0)终止反应。通过Dowex阳离子交换色谱法分离游离无机磷酸盐，并如所述通过闪烁计数进行定量。 |
| Data Literature Source | [1]. Handschumacher RE，et al. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984 Nov 2;226(4674):544-7. [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. [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. [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. [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. [6]. Borel JF，et al. Effects of the new anti-lymphocytic peptide cyclosporin A in animals. Immunology. 1977 Jun;32(6):1017-25. [7]. Williams，R，et al. Randomised trial comparing tacrolimus (FK506) and cyclosporin in prevention of liver allograft rejection. European FK506 Multicentre Liver Study Group. Lancet，1994，344(8920)，423-428. |
| Unit | Bottle |
| Specification | 20mg 10mM*1mL in DMSO 100mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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