Биологическая активность
A-552 (A552) is a мощный, малая молекула антагонист of human IL-36γ, exhibits Ki of 31/54 nM in the human IL-36γ evoked CXCL1 release in human/mouse клеточный assays.A-552 directly binds to human IL-36γ с IC50 of 67.6 nM measured by ITC, does not show affinity for either mouse IL-36γ, human IL-36α or IL-36β.A-552 attenuates human IL-36γ induced chemokine release in mouse plasma, and hIL-36γ induced inflammation in human 3D skin equivalents.A-552 is a novel first in class малая молекула антагонист of the IL-36 signaling pathway that binds селективный human IL-36γ and can dose-dependently inhibit IL-36γ induced production of proinflammatory cytokines from human and mouse cells.
Оригинал на английском
A-552 (A552) is a potent, small molecule antagonist of human IL-36γ, exhibits Ki of 31/54 nM in the human IL-36γ evoked CXCL1 release in human/mouse cellular assays.A-552 directly binds to human IL-36γ with IC50 of 67.6 nM measured by ITC, does not show affinity for either mouse IL-36γ, human IL-36α or IL-36β.A-552 attenuates human IL-36γ induced chemokine release in mouse plasma, and hIL-36γ induced inflammation in human 3D skin equivalents.A-552 is a novel first in class small molecule antagonist of the IL-36 signaling pathway that binds selective human IL-36γ and can dose-dependently inhibit IL-36γ induced production of proinflammatory cytokines from human and mouse cells.
Химические свойства
- Брутто-формула
- C₂₉H₂₉N₃O₄
- Мол. масса
- 483.57 г/моль
- Синонимы
- A552
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.