Биологическая активность
LY2775240 (LY-2775240) is a highly селективный, мощный and orally active ингибитор of phosphodiesterase 4 (PDE4) с IC50 of 0.09/0.09/2.4/0.14 nM for PDE4A/B/C/D.LY2775240 displays >200-fold selectivity over PDE10A, and >5000-fold selectivity over other PDE isoforms (IC50>10 uM).LY2775240 potently inhibits TNFα secreted induced by Toll‐like рецептор 4 агонист LPS in a human whole blood assay, inhibited LPS‐stimulated TNFα but has no effect with the media‐only control.LY2775240 is more мощный than apremilast (IC50, 18 nM vs. 290 nM), also affects E‐selectin, secreted IgG, plasminogen activator ингибитор‐1, and secreted IL‐10.
Оригинал на английском
LY2775240 (LY-2775240) is a highly selective, potent and orally active inhibitor of phosphodiesterase 4 (PDE4) with IC50 of 0.09/0.09/2.4/0.14 nM for PDE4A/B/C/D.LY2775240 displays >200-fold selectivity over PDE10A, and >5000-fold selectivity over other PDE isoforms (IC50>10 uM).LY2775240 potently inhibits TNFα secreted induced by Toll‐like receptor 4 agonist LPS in a human whole blood assay, inhibited LPS‐stimulated TNFα but has no effect with the media‐only control.LY2775240 is more potent than apremilast (IC50, 18 nM vs. 290 nM), also affects E‐selectin, secreted IgG, plasminogen activator inhibitor‐1, and secreted IL‐10.
Химические свойства
- CAS №
- 1628160-15-5
- Брутто-формула
- C₂₆H₃₅N₃O₆
- Мол. масса
- 485.58 г/моль
- Синонимы
- LY-2775240
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.