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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].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | Backorder |
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]. |
Targets&IC50 | HCV NS3 protease:6.7 nM |
In vitro | BI-1230 demonstrates potent activity in biochemical and cellular assays. With a 60-minute incubation, it exhibits an IC50 value of 6.7 nM in an enzymatic assay[1]. Over 72 hours, BI-1230 shows EC50 values of 4.6 nM and <1.8 nM in a cell-based HCVPV RNA replication luciferase reporter assay with genotype backgrounds 1a and 1b, respectively, 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%. |
Molecular Weight | 816.96 |
Formula | C42H52N6O9S |
Cas No. | 849022-32-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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