Биологическая активность
MF-766 (MF766) is a highly мощный and селективный EP(4) антагонист with связывание Ki of 0.23 nM, displays no significant affinity (>7000-fold selectivity) against other PG receptors (IC50>1500 nM); behaved as a full антагонист with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay; exhibits blockade of inhibition of TNFa-induced IP10 release by the specific EP4 агонист L-000902688 (IC50=9.5 nM); demonstrates potency and efficacy of in the rat AIA model measuring inhibition of paw swelling.
Оригинал на английском
MF-766 (MF766) is a highly potent and selective EP(4) antagonist with binding Ki of 0.23 nM, displays no significant affinity (>7000-fold selectivity) against other PG receptors (IC50>1500 nM); behaved as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay; exhibits blockade of inhibition of TNFa-induced IP10 release by the specific EP4 agonist L-000902688 (IC50=9.5 nM); demonstrates potency and efficacy of in the rat AIA model measuring inhibition of paw swelling.
Химические свойства
- CAS №
- 1050656-06-8
- Брутто-формула
- C₂₇H₂₁F₃N₂O₃
- Мол. масса
- 478.47 г/моль
- SMILES
- O=C(O)C1=CC=C(C2(NC(C3=CC=CC4=C3N(CC5=CC=C(C(F)(F)F)C=C5)C=C4)=O)CC2)C=C1
- Синонимы
- MF-766|MF766; MF 766
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: Colucci J, et al. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3760-3. View Related Products by Target Prostaglandin Receptor
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.