Биологическая активность
GSK812397 is a мощный, селективный, noncompetitive, orally available антагонист of CXCR4 рецептор, inhibits entry of X4-tropic strains of HIV-1 с IC50 of 4.60 nM and 1.50 nM in PBMCs and HOS assays, respectively; does not block CCR5-mediated viral entry in the R5 viral HOS assay (IC50>25 uM); produces a concentration-dependent decrease in both an SDF-1-mediated chemotaxis and intracellular calcium release (IC50=0.34 nM and 2.41 nM, respectively) in клетка-based functional assays; demonstrates antiviral activity against a broad range of X4-utilizing strains of HIV-1.
Оригинал на английском
GSK812397 is a potent, selective, noncompetitive, orally available antagonist of CXCR4 receptor, inhibits entry of X4-tropic strains of HIV-1 with IC50 of 4.60 nM and 1.50 nM in PBMCs and HOS assays, respectively; does not block CCR5-mediated viral entry in the R5 viral HOS assay (IC50>25 uM); produces a concentration-dependent decrease in both an SDF-1-mediated chemotaxis and intracellular calcium release (IC50=0.34 nM and 2.41 nM, respectively) in cell-based functional assays; demonstrates antiviral activity against a broad range of X4-utilizing strains of HIV-1.
Химические свойства
- CAS №
- 878197-98-9
- Брутто-формула
- C₂₄H₃₂N₆O
- Мол. масса
- 420.56 г/моль
- Синонимы
- GSK 812397; GSK-812397
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.