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产品介绍
产品介绍
产品信息
抗原名称
HCV NS3-4A serine protease
商品描述
Telaprevir (VX-950)是一种丙型肝炎病毒(HCV)NS3-4A丝氨酸蛋白酶抑制剂，IC50为0.354 μM。Telaprevir 作用于Con1(基因型 1b) 亚基因组HCV复制细胞，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 显著促进对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，这种作用存在时间依赖性。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。
分子量
679.85
纯度
98%
可溶性
DMSO ：125 mg/mL (183.9 mM)
In vitro(体外研究)
Telaprevir inhibits the hepatitis C virus NS3-4A serine protease, leading to the block of viral polyprotein processing and subsequently decrease of viral RNA replication, total HCV RNA levels and protein levels in the Con1 (genotype 1b) subgenomic HCV replicon cells in a time- and dose-dependent manner. Telaprevir displays a significant time-dependent increase in inhibitory effect on the replication of HCV RNA with IC50 values of 0.574 μM, 0.488 μM, 0.210 μM and 0.139 μM for 24, 48, 72 and 120 hours incubation, respectively. Telaprevir displays an average IC50 of 0.354 μM and an average IC90 of 0.830 μM, respectively, from three independent experiments using the 48 hours incubation. Telaprevir has no significant cytotoxicity to HCV replicon cells, parental Huh-7 and HepG2 cells after 48 hours incubation. Telaprevir (17.5 μM) completely eradicates HCV RNA from replicon cells after 13 days incubation without rebound after Telaprevir is withdrawn. Telaprevir displays an additive to moderate synergistic effect on reduction of HCV RNA replication and suppression of resistance mutations without significant increase in cytotoxicity when in combination with IFN-α, compared to treatment with each agent alone.
In vivo(体内研究)
Oral administration of Telaprevir reduces HCV protease-dependent cleavage and subsequent secretion of SEAP from the liver into the blood in the mice model to 18.7% and 18.4% at dosage of 10 and 25 mg/kg, respectively. Administration of Telaprevir at 200 mg/kg for 1 week results in a 1.9 log reduction of HCV RNA in genotype 1b HCV-infected human hepatocyte chimeric mice, and when treatment in combination with MK-0608 (50 mg/kg) for 4 weeks, viruses are eliminated from mice.
背景
别名
VX-950；特拉普韦
分子式
C36H53N7O6
CAS号
402957-28-2
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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