| Description | Telaprevir (Incivek) (VX-950) is an effective inhibitor of HCV NS3-4A serine protease (IC50: 0.35 μM). |
| In vitro | 在小鼠模型中, Telaprevir（10和25 mg/kg,p.o.） 降低丙型肝炎病毒蛋白酶依赖的裂解（18.7%）和SEAP（18.4%）从肝脏到血液的分泌中.在基因型1b HCV感染人肝细胞的小鼠中,Telaprevir（200 mg/kg）处理1周可使HCV RNA降低,和MK-0608（50 mg/kg）联用处理小鼠,持续4周,可完全除去鼠体内病毒. |
| In vivo | Telaprevir （17.5 μM）完全消除复制细胞中HCV RNA,停止处理13天后也不再出现。Telaprevir和IFN-α联用可适度提高协同作用,降低HCV RNA复制并抑制耐药突变,但无明显毒性。Telaprevir时间依赖性地促进对HCV RNA复制的抑制,温育24, 48, 72和120小时,则IC50值分别为 0.574 μM, 0.488 μM, 0.210 μM和0.139 μM。在Con1(基因型 1b) 亚基因组HCV复制细胞中,Telaprevir抑制丙型肝炎病毒NS3-4A丝氨酸蛋白酶,导致病毒多聚蛋白加工受抑制,且随后使病毒RNA复制,全部HCV RNA水平和蛋白水平降低,这种作用存在时间和剂量依赖性。Telaprevir处理HCV复制细胞,亲本Huh-7和HepG2细胞48小时后,对细胞没有毒性。 |
| Cell experiments | Cells are incubated with various concentrations of Telaprevir for 48 hours. Cell viability is determined by using a tetrazolium (MTS)-based cell viability assay.(Only for Reference) |
| Target activity | HCV NS3/4A serine protease:0.35 μM |
| Synonyms | VX-950, LY-570310, Incivek, MP-424, 特拉匹韦 |
| molecular weight | 679.85 |
| Molecular formula | C36H53N7O6 |
| CAS | 402957-28-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (183.9 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Lin K, et al. Antimicrob Agents Chemother, 2006, 50(5), 1813-1822. 2. Perni RB, et al. Antimicrob Agents Chemother, 2006, 50(3), 899-909. 3. Ohara E, et al. J Hepatol, 2011, 54(5), 872-878. |