Биологическая активность
DF2593A (DF 2593A) is a мощный, селективный, noncompetitive allosteric ингибитор of C5aR с IC50 of 5 nM (C5a-induced human PMN migration inhibition), and rat and mouse orthologs (IC50=6.0 nM and IC50=1.0 nM, respectively); dispalys >1,000-fold селективный versus other chemoattractants, including CXCL8 and CXCL1 (CI50>10 uM), as well as on a panel of different GPCRs and ion channels; DF2593A demonstrated antinociceptive effects in several models of inflammatory pain and effectively inhibited articular hyperalgesia in CFA-induced mechanical and thermal hyperalgesia and arthritic nociception.
Оригинал на английском
DF2593A (DF 2593A) is a potent, selective, noncompetitive allosteric inhibitor of C5aR with IC50 of 5 nM (C5a-induced human PMN migration inhibition), and rat and mouse orthologs (IC50=6.0 nM and IC50=1.0 nM, respectively); dispalys >1,000-fold selective versus other chemoattractants, including CXCL8 and CXCL1 (CI50>10 uM), as well as on a panel of different GPCRs and ion channels; DF2593A demonstrated antinociceptive effects in several models of inflammatory pain and effectively inhibited articular hyperalgesia in CFA-induced mechanical and thermal hyperalgesia and arthritic nociception.
Химические свойства
- CAS №
- 2351103-43-8
- Брутто-формула
- C₁₈H₂₆ClF₃N₂O₄S
- Мол. масса
- 458.92 г/моль
- Синонимы
- DF 2593A
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.