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Pirfenidone

吡非尼酮,S-7701,AMR-69

Pirfenidone抑制TGF-β产生和TGF-β刺激的胶原蛋白产生，且降低TNF-α和IL-1β产量，具有抗纤维化和抗炎特性。

目录号
EY0787
EY0787
EY0787
EY0787
纯度
99.55%
99.55%
99.55%
99.55%
规格
25 mg
100 mg
200 mg
500 mg
原价
300
500
720
1020
售价
300
500
720
1020
库存
现货
现货
现货
现货
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  • 生物活性

    Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. In pulmonary fibrosis studies, Pirfenidone is shown to block collagen production and mitigate the presentation of bleomycin- and cyclophosphamide-induced fibrosis. This intervention appears in part on the transcriptional level, with Pirfenidone exposure correlating to a significant decrease in levels of procollagen I and III gene-assoicated messenger RNA.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    250 mg/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] Nakazato H, et al. Eur J Pharmacol, 2002, 446(1-3), 177-185.
    [2] Kehrer, J.P. and Margolin, S.B. 1997. Toxicol. Lett. 90: 125-132.
    [3] Lee, B.S., et al. 1998. J. Clin. Endocrinol. Metab. 83: 219-223.
    [4] Giri, S.N., et al. 1999. J. Environ. Pathol. Toxicol. Oncol. 18: 169-177.
    [5] Iyer, S.N., et al. 1999. J. Pharmacol. Exp. Ther. 289: 211-218.
    [6] Mei, S., et al. 2005. J. Pharmacol. Exp. Ther. 313: 379-388.

    分子式
    C12H11NO    		 分子量
    185.22    		 CAS号
    53179-13-8    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >20 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    >20 mg/mL

    体内溶解度

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

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02408744 Fibrosis|Chronic Kidney Disease Drug: Pirfenidone University of Guadalajara|Cell Therapy And Technology, S.a. De C.v. Phase 1|Phase 2 2009-09-01 2015-04-02
    NCT02598193 Idiopathic Pulmonary Fibrosis Drug: Nintedanib|Drug: Pirfenidone Hoffmann-La Roche Phase 4 2016-01-14 2017-03-08
    NCT00076102 Neurofibromatosis 1|Neurofibroma, Plexiform Drug: Pirfenidone National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 2 2004-01-01 2013-03-11
    NCT02699879 Idiopathic Pulmonary Fibrosis Drug: Pirfenidone Hoffmann-La Roche 2012-02-01 2016-07-01
    NCT02262299 Disorder Related to Lung Transplantation|CLAD, Bronchiolitis Obliterans Drug: Pirfenidone|Drug: Placebo Rigshospitalet, Denmark Phase 2|Phase 3 2015-05-01 2016-12-08
    NCT02689778 Diabetic Nephropathy|Albuminuria Drug: Pirfenidone|Drug: Placebo Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran|Grupo Medifarma, S. A. de C. V. Phase 3 2016-03-01 2016-08-29
    NCT02821689 Dermatopolymyositis|Interstitial Lung Disease Drug: Pirfenidone RenJi Hospital Phase 4 2016-07-01 2016-06-30
    NCT02525484 Healthy Volunteer Drug: Pirfenidone Hoffmann-La Roche Phase 1 2015-08-01 2016-11-01
    NCT02579603 Idiopathic Pulmonary Fibrosis Drug: Nintedanib|Drug: Pirfenidone Boehringer Ingelheim Phase 4 2015-10-01 2017-01-25
    NCT02932566 Cardiac Failure Drug: Pirfenidone|Drug: Placebo University Hospital of South Manchester NHS Foundation Trust|National Institute for Health Research, United Kingdom|University of Manchester|University of Liverpool, Clinical Trials Research Centre|Roche Therapeutics Ltd Phase 2 2017-01-01 2017-01-10
    NCT02808871 Rheumatoid Arthritis Interstitial Lung Disease Drug: Pirfenidone|Drug: Placebo Ivan O. Rosas|Brigham and Women's Hospital Phase 2 2017-01-01 2016-08-17
    NCT00080223 Idiopathic Pulmonary Fibrosis|Pulmonary Fibrosis Drug: Pirfenidone Genentech, Inc. Phase 2 2003-08-01 2016-02-10
    NCT00001596 Albinism|Inborn Errors of Metabolism|Oculocutaneous Albinism|Platelet Storage Pool Deficiency|Pulmonary Fibrosis Drug: Pirfenidone|Drug: Placebo William Gahl, M.D.|National Human Genome Research Institute (NHGRI)|National Institutes of Health Clinical Center (CC) Phase 2 2005-09-01 2015-10-05
    NCT01933334 Systemic Sclerosis Drug: Pirfenidone Genentech, Inc. Phase 2 2013-10-01 2016-07-06
    NCT00063583 Diabetes Mellitus|Diabetic Nephropathy Drug: Pirfenidone Sharma, Kumar, M.D.|National Institutes of Health (NIH)|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) Phase 1|Phase 2 2003-06-01 2009-11-03
    NCT02648048 Idiopathic Pulmonary Fibrosis Drug: Pirfenidone|Drug: Vismodegib Hoffmann-La Roche Phase 1 2016-01-01 2017-02-17
    NCT00662038 Idiopathic Pulmonary Fibrosis Drug: pirfenidone Genentech, Inc.|Hoffmann-La Roche Phase 3 2008-08-01 2016-07-13
    NCT02951429 Idiopathic Pulmonary Fibrosis Drug: Pirfenidone|Drug: Placebo|Drug: Sildenafil Hoffmann-La Roche Phase 2 2017-01-13 2017-03-20
    NCT02958917 Interstitial Lung Disease Drug: Pirfenidone|Other: Placebo controlled National Jewish Health|Genentech, Inc. 2016-12-01 2016-11-04
    NCT02161952 Fibrosis|Hepatitis C Chronic Drug: Pirfenidone|Drug: Matched equivalent placebo University of Guadalajara|Cell Therapy And Technology, S.a. De C.v. Phase 2 2005-05-01 2014-07-07
    NCT02136992 Idiopathic Pulmonary Fibrosis Drug: Pirfenidone|Drug: placebo Shanghai Pulmonary Hospital, Shanghai, China|Nanjing Chia-tai Tianqing Pharmaceutical Phase 2 2011-12-01 2014-05-12
    NCT02622477 Idiopathic Pulmonary Fibrosis Drug: Pirfenidone Hoffmann-La Roche|InterMune Deutschland GmbH 2014-06-01 2017-02-26
    NCT03068234 Systemic Sclerosis Drug: Pirfenidone|Drug: Placebo oral capsule|Drug: Steroids RenJi Hospital Phase 2|Phase 3 2017-05-01 2017-02-24
    NCT00001959 Fibrosis|Focal Glomerulosclerosis|Kidney Failure|Nephrotic Syndrome|Proteinuria Drug: Pirfenidone National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) Phase 2 1999-12-01 2014-05-16

    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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