GS-9451 is a potent macrocyclic HCV NS3 PI that achieved a median maximal change in HCV RNA of 3.6 log10 IU/mL (range, -4.7 log10 to -3.1 log10 IU/mL) following 3-day monotherapy in treatment-naïve patients with HCV genotype 1 infection during phase I. In multiple GT1a and GT1b replicon cell lines, GS-9451 had mean 50% effective concentrations (EC50s) of 13 and 5.4 nM, respectively, with minimal cytotoxicity; similar potency was observed in chimeric replicons encoding the NS3 protease gene of GT1 clinical isolates. GS-9451 was less active in GT2a replicon cells (EC50 = 316 nM). GS-9451 showed good oral bioavailability in all three species tested.
CAS Number | 1310824-24-8 |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related HCV Protease Products |
---|
Hepatitis C Virus S5A/5B
Hepatitis C Virus S5A/5B is a synthetic peptide substrate. |
Ac-D-DGla-LI-Cha-C
Ac-D-DGla-LI-Cha-C is a potent HCV protease inhibitor peptide. |
Ac-EEVVAC-pNA
Ac-EEVVAC-pNA is a chromogenic substrate for a continuous spectrophotometric assay of HCV NS3 protease. |
Hepatitis Virus C NS3 Protease Inhibitor 2
Hepatitis Virus C NS3 Protease Inhibitor 2 is a product-based peptide inhibitor of hepatitis C virus (HCV) NS3 protease, with a Ki of 41 nM. |
Mipomersen
Mipomersen is a 20-base gapmer (antisense oligonucleotide) that inhibits apolipoprotein B (apoB) and lowers LDL, which can be used in studies related to hyperlipidemia. In addition, Mipomersen has anti-HCV activity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.