Биологическая активность
ARN 23746 (ARN-23746) is a мощный, селективный ингибитор of Na+-K+-Cl- importer NKCC1, shows NKCC1 inhibition 31.8% at 10 uM, and 95.2% at 100 uM in the Cl− influx assay on NKCC1-transfected HEK293 cells.ARN23746 did not show significant NKCC2 inhibition and KCC2 inhibition at 10 uM.ARN23746 selectively blocks NKCC1 in a human клетка line and restore the physiological [Cl−]i in murine DS neurons in culture, has excellent solubility and metabolic stability, and displays no issues with off-target activity in vitro.ARN23746 demonstrated in vivo efficacy in rescuing cognitive impairment in a DS mouse model and social deficits and repetitive behaviors in an autism mouse model.
Оригинал на английском
ARN 23746 (ARN-23746) is a potent, selective inhibitor of Na+-K+-Cl- importer NKCC1, shows NKCC1 inhibition 31.8% at 10 uM, and 95.2% at 100 uM in the Cl− influx assay on NKCC1-transfected HEK293 cells.ARN23746 did not show significant NKCC2 inhibition and KCC2 inhibition at 10 uM.ARN23746 selectively blocks NKCC1 in a human cell line and restore the physiological [Cl−]i in murine DS neurons in culture, has excellent solubility and metabolic stability, and displays no issues with off-target activity in vitro.ARN23746 demonstrated in vivo efficacy in rescuing cognitive impairment in a DS mouse model and social deficits and repetitive behaviors in an autism mouse model.
Химические свойства
- CAS №
- 2497525-96-7
- Брутто-формула
- C₁₇H₂₅F₃N₂O₄S
- Мол. масса
- 410.45 г/моль
- SMILES
- O=C(O)C1=CC(S(=O)(N(C)C)=O)=C(NCCCCCCCC(F)(F)F)C=C1
- Синонимы
- ARN-23746
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 Publication: 1. Savardi A, et al. Chem. 2020 Aug 6;6(8):2073-2096. 2. Borgogno M, et al. J Med Chem. 2021 Jul 22;64(14):10203-10229
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.