Биологическая активность
CCR7 ингибитор Cmp1205 is an allosteric лиганд and антагонист for human CC chemokine рецептор 7 (CCR7) with Kd of 3 nM, suppresses arrestin связывание in response to activation by CCL19 с IC50 of 7.3 uM.Cmp1205 binds to a pocket at the intracellular part of CCR7 between the ends of TM1, TM2, TM3, and TM6 and the loop between TM7 and H8.Cmp1205 allosterically inhibits связывание of the native chemokine CCL19 лиганд in a membrane-based competition связывание experiment с IC50 of 35 nM.
Оригинал на английском
CCR7 inhibitor Cmp1205 is an allosteric ligand and antagonist for human CC chemokine receptor 7 (CCR7) with Kd of 3 nM, suppresses arrestin binding in response to activation by CCL19 with IC50 of 7.3 uM.Cmp1205 binds to a pocket at the intracellular part of CCR7 between the ends of TM1, TM2, TM3, and TM6 and the loop between TM7 and H8.Cmp1205 allosterically inhibits binding of the native chemokine CCL19 ligand in a membrane-based competition binding experiment with IC50 of 35 nM.
Химические свойства
- CAS №
- 681514-83-0
- Брутто-формула
- C₂₂H₂₉N₅O₅S
- Мол. масса
- 475.56 г/моль
- Синонимы
- Cmp2105; CCR7 Ligand 1; CCR7-inhibitor-Cmp1205; CCR7-Ligand-1
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.