Boceprevir (EBP-520, SCH503034) is an HCV protease inhibitor (Ki=14 nM) for the treatment of hepatitis C virus infection. Boceprevir with pegylated interferon and ribavirin (PegIFN/RBV) enabled improvement in sustained virological response rates of patients with genotype 1 HCV. Boceprevir interacts with immunosuppressive therapy (IT) by inhibiting the cytochrome P450 3A enzyme.
| Molecular Weight | 519.68 |
| Formula | C27H45N5O5 |
| CAS Number | 394730-60-0 |
| Solubility (25°C) | DMSO 15 mg/mL |
| Storage | -20°C, protect from light, sealed |
| 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. |
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