BI-1230 

BI-1230 is potent and 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].

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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, V_ss: 2.05 L/kg^[1].
BI-1230 (oral administation; 5 mg/kg) shows good PK activity in rat: T_1/2: 2.1 hours; T_max: 1.8 nM; C_max: 405 nM; AUC0-inf: 2550 nM*h; F: 42%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

816.96

C₄₂H₅₂N₆O₉S

849022-32-8

O=C([C@]([C@]1([H])/C=C\CCCCC[C@@H]2NC(OC3CCCC3)=O)(C1)NC([C@@](C[C@@H](OC4=CC(C5=CSC(NC(C(C)C)=O)=N5)=NC6=C(C)C(OC)=CC=C46)C7)([H])N7C2=O)=O)O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

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