Биологическая активность
Lenacapavir, also known as GS-6207, is a HIV-1 capsid ингибитор. Lenacapavir shows anti-HIV activity. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs). Lenacapavir demonstrated picomolar potency in vitro with no cross resistance to existing antiretroviral classes and мощный antiviral activity in persons with HIV-1. In persons with HIV-1, there was no preexisting resistance to lenacapavir regardless of treatment history.
Оригинал на английском
Lenacapavir, also known as GS-6207, is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs). Lenacapavir demonstrated picomolar potency in vitro with no cross resistance to existing antiretroviral classes and potent antiviral activity in persons with HIV-1. In persons with HIV-1, there was no preexisting resistance to lenacapavir regardless of treatment history.
Химические свойства
- CAS №
- 2189684-44-2
- Брутто-формула
- C₃₉H₃₂ClF₁₀N₇O₅S₂
- Мол. масса
- 968.28 г/моль
- SMILES
- ClC1C([H])=C([H])C(=C2C=1C(N([H])S(C([H])([H])[H])(=O)=O)=NN2C([H])([H])C(F)(F)F)C1C([H])=C([H])C(C#CC(C([H])([H])[H])(C([H])([H])[H])S(C([H])([H])[H])(=O)=O)=NC=1[C@]([H])(C([H])([H])C1C([H])=C(C([H])=C(C=1[H])F)F)N([H])C(C([H])([H])N1C2=C(C(C(F)(F)F)=N1)[C@@]1([H])C([H])([H])[C@@]1([H])C2(F)F)=O
- Синонимы
- A9A0O6FB4H; GS-CA1; N-[(1S)-1-[3-[4-chloro-3-(methanesulfonamido)-1-(2,2,2-trifluoroethyl)indazol-7-yl]-6-(3-methyl-3-methylsulfonyl-but-1-ynyl)-2-pyridyl]-2-(3,5-difluorophenyl)ethyl]-2-[difluoro(trifluoromethyl)[?]yl]acetamide; N-((S)-1-(3-(4-Chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3-(trifl; Unii-A9A0O6FB4H и ещё 2
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.