| Description | BI-1230 is a potent inhibitor of HCV NS3 protease, exhibiting efficacy in the low nanomolar range, and notably suppresses viral replication. This compound demonstrates high selectivity, distinguishing effectively between other serine/cysteine proteases. Additionally, BI-1230 exhibits favorable pharmacokinetic (PK) properties[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. |
| In vivo | 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%. |
| Target activity | HCV NS3 protease:6.7 nM |
| molecular weight | 816.96 |
| Molecular formula | C42H52N6O9S |
| CAS | 849022-32-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |