Биологическая активность
RS-1269 is a highly мощный, селективный CCR4 антагонист, inhibits [125I]CCL17 связывание to human CCR4 с IC50 of 27.7 nM.RS-1269 also has strong affinity to displace the CCL17 связывание с IC50 of 27.0 nM in CCR4-expressing CHO cells.RS-1269 displays no competitive displacement in the связывание of [125I]CCL3 (MIP-1α) to CCR1 and [125I]CCL2 (MCP-1) to CCR2b.RS-1269 dose-dependently inhibited CCL17-induced migration of Th2 cells с IC50 of 5.5 nM.Orally administered RS-1269 (30 mg/kg) ameliorates ovalbumin-induced ear swelling in mice.RS-1269 also inhibited LPS-induced TNF-α production in vivo.
Оригинал на английском
RS-1269 is a highly potent, selective CCR4 antagonist, inhibits [125I]CCL17 binding to human CCR4 with IC50 of 27.7 nM.RS-1269 also has strong affinity to displace the CCL17 binding with IC50 of 27.0 nM in CCR4-expressing CHO cells.RS-1269 displays no competitive displacement in the binding of [125I]CCL3 (MIP-1α) to CCR1 and [125I]CCL2 (MCP-1) to CCR2b.RS-1269 dose-dependently inhibited CCL17-induced migration of Th2 cells with IC50 of 5.5 nM.Orally administered RS-1269 (30 mg/kg) ameliorates ovalbumin-induced ear swelling in mice.RS-1269 also inhibited LPS-induced TNF-α production in vivo.
Химические свойства
- CAS №
- 1310462-38-4
- Брутто-формула
- C₃₅H₃₈N₄O₃
- Мол. масса
- 562.71 г/моль
- Синонимы
- RS1269
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.