Биологическая активность
SRI-22136 is a Delta Opioid рецептор (DOR) антагонист that can cross blood-brain barrier with a IC50 of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC50 = 370 nM), KOR (IC50 = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR агонист)) (IC50 = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease.
Оригинал на английском
SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC50 of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC50 = 370 nM), KOR (IC50 = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist)) (IC50 = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease.
Химические свойства
- Брутто-формула
- C₃₀H₂₉ClN₂O₃
- Мол. масса
- 501.02 г/моль
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.