包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cell lines | Huh7-Luc HCV genotype 1b replicon cell line |
Preparation method | The solubility of this compound in DMSO is >18.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ for several months. |
Reacting condition | 0.1 ~ 1000 nM; 72 hrs |
Applications | In Huh7-Luc HCV genotype 1b replicon cell line, Simeprevir exhibited dose-dependent inhibitory effects, with the EC50 and EC90 values of 8 nM and 24 nM, respectively. Meanwhile, Simeprevir did not show significant effect on the cellular ribosomal protein RPL13A transcript level. According to the immunoblot analysis of replicon cell lysates collected after 72 hrs, NS5B expression was dose-dependently reduced, but α-tubulin expression was not suppressed. |
Animal models | Male SD rats |
Dosage form | 2 mg/kg, i.v. or 20 mg/kg, p.o. |
Applications | In male SD rats, Simeprevir was well distributed in the liver, with a high liver/plasma ratio after oral administration reaching 32. The T1/2 value for oral administration of Simeprevir was 2.8 hrs. When Simeprevir was given intravenously, Simeprevir showed a low clearance (Cl = 0.505 L/h/kg) associated with a low Vdss (0.490 L/kg). |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
产品描述 | Simeprevir is a potent inhibitor of HCV NS3/4A protease with Ki value of 0.36 nM [1]. |