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Telaprevir

CAS No. : 402957-28-2

MCE 国际站：Telaprevir

产品活性：Telaprevir (VX-950) 是一种有效的选择性的可逆 HCV NS3-4A protease 抑制剂，作用于基因 1型 (H株) NS3 蛋白酶结构域和 NS4A 辅因子肽，K_i 为 7 nM。Telaprevir 抑制 SARS-CoV-2 3CL^pro 活性。

研究领域：Anti-infection  |  Metabolic Enzyme/Protease

作用靶点：HCV Protease  |  HCV  |  SARS-CoV

In Vitro: Telaprevir (VX-950) is a covalent, reversible inhibitor of the NS3-4A protease with a slow-binding and slow-dissociation mechanism. Telaprevir exhibits significantly different kinetics in enzyme inhibition, which is most clearly exemplified by a very long half-life (58 min) of the bound enzyme-inhibitor complex. Telaprevir is additive to moderately synergistic with IFN-α in inhibiting HCV replication and in suppressing the emergence of resistance in replicon cells. Telaprevir reduces HCV RNA levels in a time- and dose-dependent manner. The IC₅₀s following a 24, 48, 72, and 120 h incubation with Telaprevir are determined to be 0.574, 0.488, 0.21, and 0.139 μM, respectively, indicating an increase in inhibitory effects with time. Following three independent experiments using the 48 h incubation in the presence of 2% FBS, the average IC₅₀ of Telaprevir is determined to be 0.354 ± 0.035 μM, and the average IC₉₀ is 0.830 ± 0.190 μM. Telaprevir (VX-950) is a potent, selective, peptidomimetic inhibitor of the hepatitis C virus (HCV) NS3-4A serine protease, and Telaprevir demonstrates excellent antiviral activity both in genotype 1b HCV replicon cells (IC₅₀=354 nM) and in human fetal hepatocytes infected with genotype 1a HCV-positive patient sera (IC₅₀=280 nM).

In Vivo: There is an ~5-fold reduction of serum SEAP activity in mice dosed with Telaprevir (VX-950) at either 10 or 25 mg/kg, which has an average value (±SEM) of 18.7±8.3% or 18.4±5.4%, respectively, compare to those administered vehicle (100±28%). These data demonstrates that Telaprevir is able to inhibit the HCV NS3-4A serine protease activity in mouse liver and block cleavage and subsequent secretion of SEAP into blood circulation in these mice.

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