Paritaprevir 是一种口服生物可利用的合成酰基磺酰胺抑制剂,可抑制丙型肝炎病毒 (HCV) 蛋白酶复合物,由非结构蛋白 3 和 4A (NS3/NS4A) 组成,对 HCV 基因型 1 具有潜在活性。 给药后,paritaprevir 可逆地结合 HCV NS3/NS4A 蛋白酶的活性中心和结合位点,并阻止 NS3/NS4A 蛋白酶介导的多蛋白成熟。这会破坏病毒蛋白的加工和病毒复制复合物的形成,从而抑制病毒在 HCV 基因型 1 感染的宿主细胞中的复制。 NS3 是一种丝氨酸蛋白酶,对于 HCV 多蛋白内多个位点的蛋白水解切割至关重要,并且在 HCV 核糖核酸 (RNA) 复制过程中起关键作用。 NS4A 是 NS3 的激活因子。 HCV 是属于黄病毒科的一种小的、有包膜的单链 RNA 病毒,感染与肝细胞癌 (HCC) 的发展有关。
产品描述
Paritaprevir is an orally bioavailable, synthetic acylsulfonamide inhibitor of the hepatitis C virus (HCV) protease complex comprised of non-structural protein 3 and 4A (NS3/NS4A), with potential activity against HCV genotype 1. Upon administration, paritaprevir reversibly binds to the active center and binding site of the HCV NS3/NS4A protease and prevents NS3/NS4A protease-mediated polyprotein maturation. This disrupts both the processing of viral proteins and the formation of the viral replication complex, which inhibits viral replication in HCV genotype 1-infected host cells. NS3, a serine protease, is essential for the proteolytic cleavage of multiple sites within the HCV polyprotein and plays a key role during HCV ribonucleic acid (RNA) replication. NS4A is an activating factor for NS3. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family, and infection is associated with the development of hepatocellular carcinoma (HCC).
体外活性
Paritaprevir demonstrates in vitro antiviral activity against HCV GT1-4 and GT6 (EC50 range, 0.09 to 19 nM), with an EC50 of 0.09 nM against GT4a[2].
Cas No.
1221573-85-8
分子式
C40H43N7O7S
分子量
765.89
别名
帕利瑞韦;Veruprevir;ABT-450
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years