Биологическая активность
BDM44768 (BDM 44768) is a мощный, селективный catalytic site ингибитор of insulin-degrading enzyme (IDE) с IC50 of 60 nM (hIDE). BDM44768 displays excellent selectivity over a panel of metalloproteases (>45-fold selectivity over hNEP and hECE, no significant acitivity against hACE and hMMP-1). BDM44768 significantly increased concentrations of Aβ1-40 in culture supernatants of human SY5Y neuroblastoma cells. Acute treatment of mice with BDM44768 (50 mg/kg, i.p.) increases insulin signalling and surprisingly impairs glucose tolerance in an IDE-dependent manner in C57BL/6J mice.
Оригинал на английском
BDM44768 (BDM 44768) is a potent, selective catalytic site inhibitor of insulin-degrading enzyme (IDE) with IC50 of 60 nM (hIDE). BDM44768 displays excellent selectivity over a panel of metalloproteases (>45-fold selectivity over hNEP and hECE, no significant acitivity against hACE and hMMP-1). BDM44768 significantly increased concentrations of Aβ1-40 in culture supernatants of human SY5Y neuroblastoma cells. Acute treatment of mice with BDM44768 (50 mg/kg, i.p.) increases insulin signalling and surprisingly impairs glucose tolerance in an IDE-dependent manner in C57BL/6J mice.
Химические свойства
- Брутто-формула
- C₂₄H₂₂FN₅O₃
- Мол. масса
- 447.47 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.