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Telaprevir

特拉匹韦,LY-570310,MP-424,VX-950,LY 570310,LY570310,MP424,MP 424

Telaprevir是一种丙型肝炎病毒(HCV)NS3-4A丝氨酸蛋白酶抑制剂，IC50为0.354 μM。

目录号
EY0369
EY0369
EY0369
纯度
99.62%
99.62%
99.62%
规格
5 mg
10 mg
50 mg
原价
990
1500
4700
售价
990
1500
4700
库存
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Telaprevir (VX-950) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    1 mM

  • 动物实验

    300 mg/kg 口服饲喂

  • 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] Lin K, et al. Antimicrob Agents Chemother, 2006, 50(5), 1813-1822.
    [2] Xia Luo,et al. Effect of Telaprevir on the Pharmacokinetics of Buprenorphine in Volunteers on Stable Buprenorphine/Naloxone Maintenance Therapy. Antimicrob Agents Chemother. 2012 Jul; 56(7): 3641–3647. doi: 10.1128/AAC.00077-12.
    [3] Varun Garg,et al. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteers. Br J Clin Pharmacol. 2013 Feb; 75(2): 431–439. Published online 2012 May 29. doi: 10.1111/j.1365-2125.2012.04345.x.

    分子式
    C36H53N7O6    		 分子量
    679.85    		 CAS号
    402957-28-2    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    136 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

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

    NCT01600976 Hepatic Impairment Drug: telaprevir Janssen Infectious Diseases BVBA Phase 1 2012-06-01 2013-11-08
    NCT01646489 Hepatitis C|Chronic Hepatitis C Drug: Miravirsen sodium|Drug: Telaprevir Santaris Pharma A/S Phase 1 2012-06-01 2012-11-09
    NCT00933283 Healthy Participants Drug: Telaprevir|Drug: Methadone Tibotec BVBA|Vertex Pharmaceuticals Incorporated Phase 1 2009-07-01 2012-11-30
    NCT00561015 Hepatitis C, Chronic Drug: Telaprevir|Drug: Peg-IFN-alfa-2a + Ribavirin (Standard Treatment)|Drug: Placebo Tibotec BVBA Phase 2 2007-12-01 2013-06-07
    NCT00775125 Hepatitis C|Telaprevir|HIV Drug: Telaprevir; Darunavir; Ritonavir; Fosamprenavir Tibotec BVBA Phase 1 2008-06-01 2010-12-16
    NCT00916474 Hepatitis C Drug: telaprevir Vertex Pharmaceuticals Incorporated|Tibotec Pharmaceutical Limited 2009-06-01 2014-02-26
    NCT01994486 Hepatitis C, Chronic Drug: Telaprevir and Sofosbuvir University of Florida|Vertex Pharmaceuticals Incorporated Phase 2 2013-12-01 2015-02-20
    NCT01841502 Hepatitis C Infection|Depression Drug: Paroxetine|Drug: telaprevir Radboud University|Janssen, LP Phase 2 2013-05-01 2014-10-27
    NCT01500616 Hepatitis C, Chronic Drug: Telaprevir|Drug: Telaprevir Janssen-Cilag International NV Phase 3 2012-06-01 2016-08-16
    NCT01332955 Hepatitis C, Chronic|HIV Infection Drug: Telaprevir|Biological: pegIFN alfa-2a|Drug: Ribavirin French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Janssen-Cilag Ltd. Phase 2 2011-04-01 2014-01-22
    NCT00903773 Hepatitis C|Kidney Diseases Drug: telaprevir Tibotec BVBA Phase 1 2009-06-01 2010-12-16
    NCT01821963 Infection Drug: Pegylated Interferon Alfa 2a|Drug: Ribavirin|Drug: Telaprevir M.D. Anderson Cancer Center|Vertex Pharmaceuticals Incorporated Phase 3 2013-04-01 2015-02-23
    NCT01054573 Hepatitis C, Chronic Drug: Telaprevir|Drug: pegylated interferon (Peg-IFN) alfa-2a|Drug: ribavirin (RBV) Janssen Infectious Diseases BVBA|Vertex Pharmaceuticals Incorporated Phase 3 2010-04-01 2013-05-06
    NCT01511432 Chronic Hepatitis C Drug: telaprevir formulation A|Drug: telaprevir Formulation B|Drug: telaprevir Formulation C|Drug: telaprevir Formulation D Vertex Pharmaceuticals Incorporated Phase 1 2012-01-01 2012-07-03
    NCT00580801 Hepatitis C Drug: Telaprevir|Drug: Pegylated-interferon-alfa-2a|Drug: Placebo|Drug: Ribavirin Tibotec BVBA Phase 2 2008-01-01 2013-08-27
    NCT01467492 Hepatitis C Drug: Telaprevir|Drug: Ribavirin|Biological: Pegylated Interferon Alfa-2a Vertex Pharmaceuticals Incorporated Phase 4 2012-01-01 2015-07-13
    NCT01890772 Hepatitis C Drug: Telaprevir|Drug: Peginterferon alfa-2a|Drug: Ribavirin|Dietary Supplement: Vitamin D Timothy Morgan, MD|Vertex Pharmaceuticals Incorporated|Southern California Institute for Research and Education Phase 2|Phase 3 2013-08-01 2014-05-13
    NCT01571583 Chronic Hepatitis C Virus (HCV) Infection Drug: Telaprevir|Drug: Pegylated interferon alfa-2a|Drug: Ribavirin Janssen-Cilag International NV Phase 3 2012-02-01 2016-06-29
    NCT01253551 Hepatitis C Drug: Treatment sequence AB|Drug: Treatment sequence BA Tibotec BVBA|Vertex Pharmaceuticals Incorporated Phase 1 2010-12-01 2012-10-13
    NCT01818856 Hepatitis C, Chronic|HIV Infection Drug: Ritonavir withdrawal, atazanavir 200 mg/12h|Drug: Telaprevir interactions Hospitales Universitarios Virgen del Roc铆o|Bristol-Myers Squibb Phase 1 2012-12-01 2013-04-19
    NCT01513941 Chronic Hepatitis C Drug: Telaprevir|Drug: Ribavirin|Drug: Pegylated-Interferon-alfa-2a Janssen-Cilag International NV Phase 3 2012-04-01 2016-05-04
    NCT02087111 Hepatitis C Drug: Telaprevir|Drug: 40 Kd Pegylated interferon alfa 2a|Drug: Ribavirin Queen Mary University of London|Janssen-Cilag Ltd.|Barts & The London NHS Trust|St George's Healthcare NHS Trust|Bradford Teaching Hospitals NHS Foundation Trust|Nottingham University Hospitals NHS Trust Phase 4 2014-04-01 2014-07-11







    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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