货号:A175194 同义名: 达匹维林 / TMC120;R147681
Dapivirine is an inhibitor of HIV reverse transcriptase with IC50 of 24 nM which is effective for many types of viruses.
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描述 | Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (4-64 μM, 24, 48, 72, 96 and 120 hours) inhibits proliferation of glioma cells and induces apoptosis (16 μM, 12-48 h). Dapivirine (8 and 16 μM, 12 h) enhances invasion of glioma cells. Dapivirine (16 μM, 12 h, 24 h and 48 h) promotes autophagy in U87 cells[3]. Dapivirine apparently blocks infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration[4]. Dapivirine is well tolerated by epithelial cells, T cells, macrophages, and cervical tissue explants with CC50 (50% cytotoxic concentration) of 10 μM to 20 μM. Dapivirine potently inhibits infection by both X4- and R5-utilizing HIV-1 strains with IC50 of 1.46 nM in cell-based assays. Dapivirine potently inhibits HIV-1BaL infection of human ectocervical explant tissue in a dose-dependent manner, as evaluated by the reduction in both p24 release and provirus content in cultured explants. Dapivirine inhibits the transmission of virus to permissive T cells in a dose-dependent manner, with an IC50 of 0.1 nM. Dapivirine results in significant inhibition of HIV infection when explants are challenged with virus immediately with IC90 of 100 nM. Dapivirine is also able to inhibit viral dissemination by migratory cells[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01755741 | Human Immunodeficiency Virus | Phase 1 | Completed | - | United States, California ... 展开 >> California Family Health Council Berkeley, California, United States, 94710 California Family Health Council Los Angeles, California, United States, 90010 收起 << |
NCT03537092 | Safety of Vaginal Film Use | Phase 1 | Recruiting | January 2019 | United States, Pennsylvania ... 展开 >> Magee womens Hospital of UPMC Recruiting Pittsburgh, Pennsylvania, United States, 15213 Contact: Ingrid Macio, PA-C 收起 << |
NCT03648931 | - | Recruiting | September 2018 | Malawi ... 展开 >> Blantyre Clinical Research Site Recruiting Blantyre, Malawi Contact: Frank Taulo, MBBS, MPH, FCOG Contact ftaulo@yahoo.com South Africa Wits Reproductive Health and HIV Institute (WRHI) Clinical Research Site Recruiting Johannesburg, South Africa Contact: Thesla Palanee-Phillips, PhD, MMedSci, MSc Contact tpalanee@whri.ac.za Uganda Makerere University - Johns Hopkins University (MU-JHU) Research Collaboration Clinical Research Site Recruiting Kampala, Uganda Contact: Juliane Etima, BSc, MA Psy Contact jetima@mujhu.org Zimbabwe Zengeza Clinical Research Site Recruiting Harare, Zimbabwe Contact: Petina Musara, BSW Contact pmusara@uzchs-ctu.org 收起 << | |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.04mL 0.61mL 0.30mL |
15.18mL 3.04mL 1.52mL |
30.36mL 6.07mL 3.04mL |
CAS号 | 244767-67-7 |
分子式 | C20H19N5 |
分子量 | 329.398 |
别名 | 达匹维林 ;TMC120;R147681 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 45 mg/mL(136.61 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |