PSI-353661  (Synonyms: GS-558093)

PSI-353661 (GS-558093) is a purine nucleotide NS5B polymerase inhibitor against HCV infection. PSI-353661 shows EC₉₀s of 8 nM and 11 nM for wild type and S282T resistant replicons of HCV. PSI-353661 can produce high concentrations of the active triphosphate in primary human hepatocytes^[1][3].

NS5B polymerase^[3]

PSI-353661 在基于细胞的复制子试验中表现出对 HCV 的强抑制作用，对野生型和 S282T 抗性复制子的 EC₉₀ 分别为 8 nM 和 11 nM^[1]。
PSI-353661 (24 小时) 在人原代肝细胞中产生高浓度 (0.44 mM) 的三磷酸盐 (TP)^[1]。
PSI-353661 (4 天) 抑制病毒复制，对基因型 1b 复制子细胞的 EC₅₀ 和 EC₉₀ 值分别为 0.0030 μM 和 0.0085 μM^[2]。
PSI-353661 (8 天) 在 Huh7、HepG2、BxPC3 和 CEM 细胞中 IC₅₀ 超过 80 μM^[2]。
PSI-353661 (8-160 nM，2 周) 可清除 HCV 复制子 RNA 并防止病毒复制^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PSI-353661 (50 mg/kg，口服，与 400 mg/kg Telaprevir (HY-10235) 联合使用，每日一次，持续 4 周) 对感染 HCV 的人肝细胞嵌合小鼠有效^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

582.52

C₂₄H₃₂FN₆O₈P

1231747-08-2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Wonsuk Chang, et al. Discovery of PSI-353661, a Novel Purine Nucleotide Prodrug for the Treatment of HCV Infection. ACS Med Chem Lett. 2010 Dec 17;2(2):130-5.  [Content Brief]

  [2]. Furman PA, et al. Activity and the metabolic activation pathway of the potent and selective hepatitis C virus pronucleotide inhibitor PSI-353661. Antiviral Res. 2011 Aug;91(2):120-32.  [Content Brief]

  [3]. Yugo Kai, et al. Emergence of hepatitis C virus NS5A L31V plus Y93H variant upon treatment failure of daclatasvir and asunaprevir is relatively resistant to ledipasvir and NS5B polymerase nucleotide inhibitor GS-558093 in human hepatocyte chimeric mice.  [Content Brief]