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Cyclosporin A

环胞霉素A,环孢素A,Cyclosporine A

Cyclosporin A 是一种免疫抑制剂，与亲环蛋白结合，且抑制calcineurin，IC50为7 nM。

目录号
EY0845
EY0845
EY0845
纯度
99.28%
99.28%
99.28%
规格
50 mg
100 mg
500 mg
原价
300
400
1000
售价
300
400
1000
库存
现货
现货
现货
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  • 生物活性

    Cyclosporin A is a potent cyclophilin inhibitor which is responsible for the opening of the MPTP (mitochondrial permeability transition pore). When tested with retinal ganglion cells, Cyclosporin A showed a high selectivity for the expression of cyclophilin D and prolonged the cells survival. In human First-Trimester Trophoblast Cells, Cyclosporin A treatment promoted cells growth and invasiveness by inhibiting Ca2+/Calcineurin/NFAT signal. Cyclosporin A treatment promoted the apoptosis of T-cell by upregulating Fas/FasL and caspase activities. Treated human T cells with Cyclosporin A suppressed T cell activation by inhibiting calcineurin and NFATc which are responsible for T cell function.

  • 体外研究

  • 体内研究

    0.5% methylcellulose+0.2% Tween 80

  • 激酶实验

  • 细胞实验

    ~100 nM

  • 动物实验

    45mg/kg 口服

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Handschumacher RE, et al. Science, 1984, 226(4674), 544-547.
    [2] Bernardi, P., et al. 1993. J. Biol. Chem. 268: 1005-1010.
    [3] Liu, J. 1993. Trends Pharmacol. Sci. 14: 182-188.
    [4] Broekemeier, K.M., et al. 1995. Biochemistry. 34: 16440-16449.
    [5] Seaton, T.A., et al. 1998. Brain Res. 809: 12-17.
    [6] Kruman, I.I. and Mattson, M.P. 1999. J. Neurochem. 72: 529-540.

    分子式
    C62H111N11O12    		 分子量
    1202.61    		 CAS号
    59865-13-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mM    		 Water
    Insoluble    		 Ethanol
    50 mM

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00983424 Metastatic Breast Cancer Drug: Cyclosporins|Drug: nab-paclitaxel Northwestern University|Avon Foundation Phase 1 2010-02-01 2013-09-13
    NCT00438360 Chronic Plaque Psoriasis Drug: Cyclosporine A microemulsion|Drug: Placebo Novartis Pharmaceuticals|Novartis Phase 3 2006-05-01 2011-07-13
    NCT01642979 Paroxysmal Nocturnal Hemoglobinuria|Hemoglobinuria|Hemoglobinuria, Paroxysmal|Proteinuria|Urination Disorders|Thrombosis|Bone Marrow Failure|Aplastic Anemia,|Anemia, Hemolytic Drug: Levamisole+cyclosporin A+Glucocorticoids|Drug: cyclosporin A+Glucocorticoids|Drug: Glucocorticoids Institute of Hematology & Blood Diseases Hospital Phase 2 2012-07-01 2013-01-01
    NCT01760096 Paroxysmal Nocturnal Hemoglobinuria|Hemoglobinuria|Hemoglobinuria, Paroxysmal|Proteinuria|Urination Disorders|Thrombosis|Bone Marrow Failure|Aplastic Anemia,|Anemia, Hemolytic Drug: Levamisole+cyclosporin A+Glucocorticoids|Drug: cyclosporin A+Glucocorticoids|Drug: Glucocorticoids Institute of Hematology & Blood Diseases Hospital Phase 2 2013-01-01 2013-01-01
    NCT00213590 Kidney Transplantation|Primary Prevention|Kidney Failure Drug: cyclosporine A University Hospital, Rouen Phase 3 2000-04-01 2012-02-14
    NCT01650662 Acute Myocardial Infarction Drug: Cyclosporine A Mario Negri Institute for Pharmacological Research|Heart Care Foundation Phase 3 2012-01-01 2015-04-15
    NCT01595958 Non Shockable Out of Hospital Cardiac Arrest Drug: Cyclosporine A|Procedure: cardio-pulmonary resuscitation Hospices Civils de Lyon Phase 3 2010-06-01 2014-04-30
    NCT00976300 Systemic Lupus Erythematosus|Lupus Nephritis Drug: Cyclosporine A|Drug: Cyclophosphamide Institute of Rheumatology, Prague|Ministry of Health, Czech Republic|Charles University, Czech Republic|Palacky University|Department of Rheumatology, Hospital, Ceske Budejovice, Czech Republic|National Institute of Rheumatology, Piestany, Slovakia|St. Anna Hospital, Brno, Czech Phase 2 2002-01-01 2010-06-22
    NCT00359814 Heart Transplantation Drug: Mycophenolatmofetile|Drug: Cyclosporin A Hannover Medical School|Hoffmann-La Roche 2004-11-01 2009-02-13
    NCT01990118 End Stage Renal Failure Drug: Neoral|Drug: Gengraf庐 capsule containing 25mg or 100mg cyclosporine Penang Hospital, Malaysia Phase 4 2004-11-01 2013-11-15
    NCT00987467 Atopic Keratoconjunctivitis Drug: Cyclosporin 0.05% ophthalmic|Drug: Cyclosporin 0.05% ophthalmic Johns Hopkins University 2007-08-01 2013-10-04
    NCT00656695 End Stage Renal Disease|Renal Transplantation Drug: Iminoral|Drug: Neoral Imam Khomeini Hospital Phase 4 2008-04-01 2012-06-21
    NCT01768312 Dry Eye Syndromes Drug: Cyclosporine ophthalmic solution Hanlim Pharm. Co., Ltd. Phase 3 2012-03-01 2013-01-11
    NCT02203422 Drug: Cyclosporin A|Drug: rhTPO Shandong University All 0 null 2014-07-01
    NCT03026946 Hand Eczema Drug: Alitretinoin|Drug: cyclosporin A University Medical Center Groningen|ZonMw: The Netherlands Organisation for Health Research and Development Phase 3 2017-03-01 2017-01-18
    NCT01990898 Interstitial Cystitis Drug: Cyclosporine The Cleveland Clinic Phase 2 2013-11-01 2016-06-14
    NCT00264355 Heart Transplantation|Acute Renal Failure Drug: cyclosporine A University of Oslo School of Pharmacy Phase 4 2005-12-01 2007-09-05
    NCT02114073 Glaucoma, Open Angle Drug: Cyclosporine|Drug: Betamethasone Mashhad University of Medical Sciences Phase 2 2014-04-01 2015-04-17
    NCT01762657 Type 1 Diabetes Drug: Oral Cyclosporine and Oral Lansoprazole|Drug: Placebos Perle Bioscience, Inc. Phase 3 2014-09-01 2016-04-17

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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