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Ledipasvir D-tartrate

CAS No. : 1502654-87-6

MCE 国际站：Ledipasvir D-tartrate

产品活性：Ledipasvir(GS5885)D-酒石酸盐是丙型肝炎NS5A蛋白抑制剂。

研究领域：Anti-infection

作用靶点：HCV

In Vitro: Ledipasvir has GT1a and 1b EC₅₀ values of 31 and 4 pM, respectively, and protein-adjusted EC₅₀ values of 210 pM (GT1a) and 27 pM (GT1b) and the intrinsic EC₅₀ of 39 is 310 fM for GT1a and 40 fM for GT1b. Ledipasvir is highly protein-bound both in human serum and in the cell-culture medium (containing 10% BSA) of the replicon assay. Ledipasvir exhibits an EC₅₀ value of 141 nM against the JFH/3a-NS5A replicon.

In Vivo: Ledipasvir is remarkable not only on the basis of its high replicon potency but also on the basis of its low clearance, good bioavailability, and long half-lives in rat, dog, and monkey and low predicted clearance in human. The pharmacokinetics of Ledipasvir is measured in rats and dogs. Ledipasvir shows good half-lives (rat 1.83 ± 0.22 hr, dog 2.63 ± 0.18 hr) in plasma, low systemic clearance (CL), and moderate volumes of distribution (Vss) that are greater than total body water volume.

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