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

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.

BI-1230 (intravenous?injection; 2 mg/kg) shows good PK activity in rat: CL: 15 ml/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%.

849022-32-8

C42H52N6O9S

816.96

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years