Биологическая активность
RTIOXA-43 is a dual orexin рецептор агонист exhibiting мощный activity at both OX1 and OX2 receptors, with EC₅₀ values of 24 nM for each . in vivo studies involving 12-month-old mice have demonstrated that peripheral administration of RTIOXA-43 significantly increases wakefulness, reduces total sleep time, and enhances sleep/wake consolidation by decreasing the number of sleep episodes and extending their duration . These findings suggest that RTIOXA-43 holds promise as a therapeutic candidate for treating orexin-deficient conditions such as narcolepsy.
Оригинал на английском
RTIOXA-43 is a dual orexin receptor agonist exhibiting potent activity at both OX1 and OX2 receptors, with EC₅₀ values of 24 nM for each . In vivo studies involving 12-month-old mice have demonstrated that peripheral administration of RTIOXA-43 significantly increases wakefulness, reduces total sleep time, and enhances sleep/wake consolidation by decreasing the number of sleep episodes and extending their duration . These findings suggest that RTIOXA-43 holds promise as a therapeutic candidate for treating orexin-deficient conditions such as narcolepsy.
Химические свойства
- CAS №
- 2832067-72-6
- Брутто-формула
- C₃₇H₃₇N₅O₅S
- Мол. масса
- 663.79 г/моль
- SMILES
- S(C1C(=CC=C(C=1)C1C=CC=C(C(N(C)CC2C=CN=CC=2)=O)C=1)OC)(NC1C=CC=C(C=1)NCCNC(C1C=CC=C(C)C=1)=O)(=O)=O
- Синонимы
- RTIOXA-43; CS-0759511; EX-A8479; HY-154789; CHEMBL5070320 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.