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Dapivirine

TMC120,TMC-120,TMC 120

Dapivirine(TMC 120, TMC 120 R147681)是HIV非核苷逆转录酶抑制剂（NNRTI），IC50为24 nM，能抑制包括NNRTI抗性的各种HIV-1毒株。

目录号
EY1608
EY1608
EY1608
99.45%
100 mg
纯度
99.45%
99.45%
99.45%
50 mg
3360
规格
5 mg
10 mg
25 mg
2400
3360
原价
520
860
1560
2400
现货
售价
520
860
1560
现货
库存
现货
现货
现货
99.45%
订购
订购
订购
订购
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  • 生物活性

    Dapivirine (TMC120) is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 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] Van Herrewege Y, et al. Antimicrob Agents Chemother, 2004, 48(1), 337-339.

    分子式
    C20H19N5    		 分子量
    329.4    		 CAS号
    244767-67-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    31 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 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
    NCT02808949 Human Immunodeficiency Virus Drug: Dapivirine International Partnership for Microbicides, Inc. Phase 1 2015-02-01 2017-03-08
    NCT02010593 Human Immunodeficiency Virus Drug: Dapivirine Vaginal Ring|Drug: Placebo Vaginal Ring International Partnership for Microbicides, Inc.|National Institute of Allergy and Infectious Diseases (NIAID) Phase 2 2013-12-01 2017-02-07
    NCT01731574 HIV Drug: dapivirine|Drug: miconazole International Partnership for Microbicides, Inc. Phase 1 2012-12-01 2013-11-06
    NCT02862171 HIV Prevention Drug: Dapivirine Vaginal Ring-004 International Partnership for Microbicides, Inc. Phase 3 2016-08-01 2016-08-05
    NCT00799058 HIV-1 Infections Drug: dapivirine|Drug: dapivirine gel 4759|Drug: Drug placebo International Partnership for Microbicides, Inc. Phase 1|Phase 2 2009-06-01 2017-01-26
    NCT03044379 HIV 1 Infection Drug: Dapivirine gel (0.05%)|Other: Universal HEC placebo gel International Partnership for Microbicides, Inc. Phase 1 2015-09-29 2017-02-06
    NCT02920827 HIV Infections Drug: dapivirine|Drug: placebo International Partnership for Microbicides, Inc. Phase 1 2009-08-01 2016-12-07
    NCT02847286 HIV- Prevention Drug: Dapivirine Ring-004|Drug: Dapivirine Ring-004 for 28 days along with clotrimazole|Drug: Clotrimazole International Partnership for Microbicides, Inc. Phase 1 2015-09-01 2016-12-16
    NCT01924091 Pharmaokinetics Drug: Dapivirine gel|Drug: Dapivirine film International Partnership for Microbicides, Inc. Phase 1 2013-09-01 2016-08-29
    NCT01277640 Topical Penile Exposures Drug: dapivirine|Drug: matched placebo|Drug: universal placebo International Partnership for Microbicides, Inc. Phase 1 2011-03-01 2015-09-09
    NCT00700284 HIV Infections Drug: placebo vaginal ring|Drug: TMC120 (dapivirine) vaginal ring International Partnership for Microbicides, Inc.|Tibotec Pharmaceutical Limited Phase 1 2004-10-01 2009-08-31
    NCT01071174 HIV Infections Other: Dapivirine|Other: Placebo International Partnership for Microbicides, Inc. Phase 1|Phase 2 2010-04-01 2011-08-01
    NCT01337583 HIV Infections Other: Dapivirine|Other: Placebo|Drug: Dapivirine International Partnership for Microbicides, Inc. Phase 3 2011-07-01 2012-06-08
    NCT01337570 HIV Infections Other: Dapivirine|Other: Placebo|Drug: Dapivirine International Partnership for Microbicides, Inc. Phase 3 2011-07-01 2012-06-08
    NCT01952561 Pharmacokinetics Drug: dapivirine ring International Partnership for Microbicides, Inc. Phase 1 2013-11-01 2016-08-25
    NCT01242579 HIV Infections Drug: Maraviroc/Dapivirine Gel|Drug: Dapivirine Vaginal Gel|Drug: Maraviroc Vaginal Gel|Drug: Matching Placebo Gel International Partnership for Microbicides, Inc. Phase 1 2011-01-01 2011-09-08
    NCT00304642 HIV Infections Drug: dapivirine (TMC120) vaginal gel International Partnership for Microbicides, Inc. Phase 1 2005-11-01 2006-06-01
    NCT02028338 Human Immunodeficiency Virus Device: placebo ring|Drug: dapivirine ring International Partnership for Microbicides, Inc.|Microbicide Trials Network|National Institutes of Health (NIH) Phase 2 2014-03-01 2017-02-09
    NCT02855346 HIV Prevention Drug: Ring 104|Drug: Ring 102 International Partnership for Microbicides, Inc.|National Institutes of Health (NIH) Phase 1 2017-04-01 2017-03-14
    NCT00917904 HIV Infections|Acquired Immunodeficiency Syndrome|Healthy Drug: dapivirine|Drug: placebo International Partnership for Microbicides, Inc. Phase 1|Phase 2 2009-07-01 2011-12-13
    NCT00332995 HIV Infections Drug: dapivirine (TMC120) vaginal ring International Partnership for Microbicides, Inc.|Tibotec Pharmaceutical Limited Phase 1 2005-07-01 2009-08-31
    NCT00917891 HIV Infections|Acquired Immunodeficiency Syndrome Drug: dapivirine|Drug: placebo International Partnership for Microbicides, Inc. Phase 1|Phase 2 2009-11-01 2011-09-09
    NCT01144676 HIV Infections Drug: dapivirine|Drug: placebo|Drug: dapivirine|Drug: placebo International Partnership for Microbicides, Inc. Phase 1 2010-04-01 2010-10-05
    NCT01539226 HIV Infections Drug: Placebo Vaginal Ring International Partnership for Microbicides, Inc. 2012-03-01 2016-12-14
    NCT01363037 HIV Infections Drug: Dapivirine Vaginal Ring|Drug: Maraviroc Vaginal Ring|Other: Placebo Vaginal Ring|Drug: Dapivirine-Maraviroc Vaginal Ring International Partnership for Microbicides, Inc. Phase 1 2011-11-01 2015-09-09

    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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