BI-1230

Names

[ Name ]:
BI-1230

Biological Activity

[Description]:

BI-1230 is potent and orally active digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity[1].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Metabolic Enzyme/Protease >> HCV Protease

[Target]

IC50: 6.7 nM (HCV NS3 protease)[1]

[In Vitro]

BI-1230 (60 min incubation) exhibits an IC50 value of 6.7 nM in a Enzymatic assay[1]. BI-1230 (72 hours) shows EC50 values of 4.6 nM and <1.8 nM in a Cell-based HCVPV RNA replication Luciferase reporter assay, genotype background 1a and 1b, in Huh7 cells[1].

[In Vivo]

BI-1230 (intravenous injection; 2mg/kg) shows good PK activity in rat: CL: 15ml/min/kg, Mean residence time after iv dose: 2.3 hours, Vss: 2.05 L/kg[1]. BI-1230 (oral administation; 5 mg/kg) shows good PK activity in rat: T1/2: 2.1 hours; Tmax: 1.8 nM; Cmax: 405 nM; AUC0-inf: 2550 nM*h; F: 42%[1].

[References]

[1]. Overview for BI-1230 an inhibitor of HCV NS3

Chemical & Physical Properties

[ Molecular Formula ]:
C₄₂H₅₂N₆O₉S

[ Molecular Weight ]:
816.96

BI-1230

Names

Biological Activity

Chemical & Physical Properties

Related Compounds