产品
编 号：F749183
分子式：C49H55ClF2N8O6
分子量：925.46
分子式：C49H55ClF2N8O6
分子量：925.46
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CAS No: 2128695-48-5
产品详情
生物活性：
Ledipasvir (GS-5885) hydrochloride is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir hydrochloride is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM.
体内研究：
Ledipasvir hydrochloride 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 hydrochloride is measured in rats and dogs. Ledipasvir shows good half-lives (rat 1.83 hr, dog 2.63hr) in plasma, low systemic clearance (CL), and moderate volumes of distribution (Vss) that are greater than total body water volume.
体外研究：
Ledipasvir hydrochloride 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 hydrochloride is highly protein-bound both in human serum and in the cell-culture medium (containing 10% BSA) of the replicon assay. Ledipasvir hydrochloride exhibits an EC50 value of 141 nM against the JFH/3a-NS5A replicon.
Ledipasvir (GS-5885) hydrochloride is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir hydrochloride is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM.
体内研究：
Ledipasvir hydrochloride 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 hydrochloride is measured in rats and dogs. Ledipasvir shows good half-lives (rat 1.83 hr, dog 2.63hr) in plasma, low systemic clearance (CL), and moderate volumes of distribution (Vss) that are greater than total body water volume.
体外研究：
Ledipasvir hydrochloride 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 hydrochloride is highly protein-bound both in human serum and in the cell-culture medium (containing 10% BSA) of the replicon assay. Ledipasvir hydrochloride exhibits an EC50 value of 141 nM against the JFH/3a-NS5A replicon.
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