Pelecopan

Modify Date: 2024-01-31 22:36:04

Pelecopan Structure
Pelecopan structure
Common Name Pelecopan
CAS Number 2378380-49-3 Molecular Weight 406.41
Density N/A Boiling Point N/A
Molecular Formula C23H19FN2O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Pelecopan


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].

 Names

Name Pelecopan

 Pelecopan Biological Activity

Description 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].
Related Catalog
Target

IC50: 14.3 nM (Complement factor D)[1]

In Vitro BCX9930 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. BCX9930 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. BCX9930 suppresses AP activity in rhesus monkeys ex vivo assays[1][3].
References

[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 2020, Pages 14-15

[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 November 2020, Page 32.

 Chemical & Physical Properties

Molecular Formula C23H19FN2O4
Molecular Weight 406.41
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