Биологическая активность
Lu AF27139 is a novel rodent-active and CNS-penetrant P2X7 рецептор антагонист. Lu AF27139 is highly селективный and мощный against rat, mouse, and human forms of the receptors. The rat pharmacokinetic profile is favorable with high oral bioavailability, modest clearance (0.79 L/(h kg)), and good CNS permeability. Importantly, Lu AF27139 was without effect in standard in vitro and in vivo toxicity studies. Lu AF27139 is a valuable tool for probing the role of the P2X7 рецептор in rodent models of CNS diseases.
Оригинал на английском
Lu AF27139 is a novel rodent-active and CNS-penetrant P2X7 receptor antagonist. Lu AF27139 is highly selective and potent against rat, mouse, and human forms of the receptors. The rat pharmacokinetic profile is favorable with high oral bioavailability, modest clearance (0.79 L/(h kg)), and good CNS permeability. Importantly, Lu AF27139 was without effect in standard in vitro and in vivo toxicity studies. Lu AF27139 is a valuable tool for probing the role of the P2X7 receptor in rodent models of CNS diseases.
Химические свойства
- CAS №
- 2097117-06-9
- Брутто-формула
- C₂₁H₁₉ClF₃N₅O₂S
- Мол. масса
- 497.92 г/моль
- SMILES
- ClC1=CC=C([C@H](N2CCOCC2)CN([H])C(C3=C(C(F)(F)F)N=C(C4=NC=CC=N4)S3)=O)C=C1
- Синонимы
- Lu AF27139
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.