Биологическая активность
BI 1265162 is a мощный ENaC ингибитор, inhibits Na+ transport с IC50 3 nM and 8 nM in M1 and NCI-H441 cells, respectively.BI 1265162 dose-dependently inhibited Na+ transport and decreased water resorption in клетка line models.BI 1265162 reduced liquid absorption in rat lungs and increased MCC in sheep, with no effects on renal function in the animal models.BI 1265162 alone and in combination with CF transmembrane conductance regulator (CFTR) modulators decreased water transport and increased MCC in both normal and CF airway human epithelial models.
Оригинал на английском
BI 1265162 is a potent ENaC inhibitor, inhibits Na+ transport with IC50 3 nM and 8 nM in M1 and NCI-H441 cells, respectively.BI 1265162 dose-dependently inhibited Na+ transport and decreased water resorption in cell line models.BI 1265162 reduced liquid absorption in rat lungs and increased MCC in sheep, with no effects on renal function in the animal models.BI 1265162 alone and in combination with CF transmembrane conductance regulator (CFTR) modulators decreased water transport and increased MCC in both normal and CF airway human epithelial models.
Химические свойства
- CAS №
- 2084037-37-4
- Брутто-формула
- C₂₆H₃₄ClF₃N₇O₇P
- Мол. масса
- 680.01 г/моль
- SMILES
- C([N+]1=C(N(CC)C2=CC=C(OCC(=O)NCCOCP(=O)(C)C)C=C12)CNC(C1=NC(Cl)=CN=C1N)=O)C.[O-]C(=O)C(F)(F)F
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.