Pelecopan (BCX9930) 是一种有效的、选择性的口服补体因子D抑制剂,IC50值为14.3 nM。Pelecopan 可靶向补体因子D以预防PNH中的血管内和血管外溶血,也可用于其他替代途径介导的疾病。
产品描述
Pelecopan (BCX9930) is a potent, selective, orally active inhibitor of complement factor D with an IC 50 value of 14.3 nM. Pelecopan can target factor D to prevent both intravascular and extravascular hemolysis in PNH. Pelecopan also be used for other alternative pathway (AP) mediated diseases [1] [2].
体外活性
BCX9930 has a potent, highly specific inhibitory activity for purified human factor D with an IC 50 value of 14.3 nM and also inhibits its proteolytic activity against factor B bound to C3b with an IC 50 of 28.1 nM. BCX9930 completely blocks hemolysis of PNH cells in vitro (with an IC 50 value of 29.5 nM in rabbit erythrocytes) and suppresses the accumulation of C3 fragments on PNH erythrocytes. BCX9930 suppresses AP activity in rhesus monkeys ex vivo assays [1] [3].
Cas No.
2378380-49-3
分子式
C23H19FN2O4
分子量
406.41
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years