For research use only. Not for therapeutic Use.
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].
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].
Catalog Number | I043393 |
CAS Number | 2378380-49-3 |
Synonyms | 2-[2-[[7-[2-(aminomethyl)-3-fluoropyridin-4-yl]-1-benzofuran-5-yl]methoxy]phenyl]acetic acid |
Molecular Formula | C23H19FN2O4 |
Purity | ≥95% |
InChI | InChI=1S/C23H19FN2O4/c24-22-17(5-7-26-19(22)12-25)18-10-14(9-16-6-8-29-23(16)18)13-30-20-4-2-1-3-15(20)11-21(27)28/h1-10H,11-13,25H2,(H,27,28) |
InChIKey | AUARNXJEAZFQCQ-UHFFFAOYSA-N |
SMILES | C1=CC=C(C(=C1)CC(=O)O)OCC2=CC(=C3C(=C2)C=CO3)C4=C(C(=NC=C4)CN)F |
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 |