Биологическая активность
HF50731 (HF-50731) is a novel мощный, селективный CXCR4 антагонист with Ki of 19.8 nM in the CXCR4 competitive связывание assay.HF50731 significantly inhibited SDF-1α-induced calcium mobilization (IC50=621 nM) and клетка migration, and blocked HIV-1 infection via antagonizing CXCR4 coreceptor function (IC50=1.5 uM).The structure-activity relationship analysis demonstrated that HF50731 could primarily occupy the minor subpocket of CXCR4 and partially bind in the major subpocket by interacting with residues W94, D97, D171, and E288.
Оригинал на английском
HF50731 (HF-50731) is a novel potent, selective CXCR4 antagonist with Ki of 19.8 nM in the CXCR4 competitive binding assay.HF50731 significantly inhibited SDF-1α-induced calcium mobilization (IC50=621 nM) and cell migration, and blocked HIV-1 infection via antagonizing CXCR4 coreceptor function (IC50=1.5 uM).The structure-activity relationship analysis demonstrated that HF50731 could primarily occupy the minor subpocket of CXCR4 and partially bind in the major subpocket by interacting with residues W94, D97, D171, and E288.
Химические свойства
- CAS №
- 2484771-19-7
- Брутто-формула
- C₂₆H₄₆N₄
- Мол. масса
- 414.68 г/моль
- Синонимы
- HF-50731
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.