Bioactivity | Pelecopan (BCX9930) is a potent, selective, orally active inhibitor of complement factor D with an IC50 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][3]. |
Target | IC50: 14.3 nM (complement factor D) |
Invitro | Pelecopan has a potent, highly specific inhibitory activity for purified human factor D with an IC50 value of 14.3 nM and also inhibits its proteolytic activity against factor B bound to C3b with an IC50 of 28.1 nM[1].Pelecopan completely blocks hemolysis of PNH cells in vitro (with an IC50 value of 29.5 nM in rabbit erythrocytes) and suppresses the accumulation of C3 fragments on PNH erythrocytes[1]. |
Name | Pelecopan |
CAS | 2378380-49-3 |
Formula | C23H19FN2O4 |
Molar Mass | 406.41 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. International Nonproprietary Names for Pharmaceutical Substances (INN) [2]. AustinKulasekararajMD MRCP, FRCPath, et al. BCX9930, a Potent, Selective, Oral Factor D Inhibitor, Demonstrates Proof-of-Concept As Monotherapy in Patients with Paroxysmal Nocturnal Hemoglobinuria (PNH). Blood (2020) Volume 136, Supplement 1, 5 November 2 [3]. XilinChenMDPhD, et al. Preclinical Characterization of BCX9930, a Potent Oral Complement Factor D Inhibitor, Targeting Alternative Pathway-Mediated Diseases Including Paroxysmal Nocturnal Hemoglobinuria (PNH). Blood (2020) Volume 136, Supplement 1, 5 Nove |