Ledipasvir-D-tartrate-GS-5885-D-tartrate-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELedipasvir D-tartrateCat. No.: HY-15602BCAS No.: 1502654-87-6Synonyms: GS-5885 D-tartrate分式: CHFNO分量: 1039.09作靶点: HCV; HCV Protease作通路: Anti-infection; Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6

2、 months-20C 1 month溶解性数据体外实验 DMSO : 28 mg/mL (26.95 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.9624 mL 4.8119 mL 9.6238 mL5 mM 0.1925 mL 0.9624 mL 1.9248 mL10 mM 0.0962 mL 0.4812 mL 0.9624 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL A

3、CTIVITY物活性 Ledipasvir(GS5885)D-酸盐 丙型肝炎NS5A蛋抑制剂。IC50 & Target EC50: 34 pM (GT1a), 4 pM (GT1b) 1体外研究Ledipasvir has GT1a and 1b EC50 values of 31 and 4 pM, respectively, and protein-adjusted EC50 values of1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE210 pM (GT1a) and 27 pM (GT1b) and the intrinsic

4、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 1. Ledipasvir exhibits an EC50 value of 141 nM against the JFH/3a-NS5A replicon 2.体内研究 Ledipasvir is remarkable not only on

5、 the basis of its high replicon potency but also on the basis of its lowclearance, good bioavailability, and long half-lives in rat, dog, and monkey and low predicted clearance inhuman. The pharmacokinetics of Ledipasvir is measured in rats and dogs. Ledipasvir shows good half-lives(rat 1.83 0.22 hr

6、, dog 2.63 0.18 hr) in plasma, low systemic clearance (CL), and moderate volumes ofdistribution (Vss) that are greater than total body water volume 1.PROTOCOLAnimal Rats, Dogs and Monkeys 1Administration 1 Pharmacokinetic studies are performed in male nave Sprague-Dawley(SD) rats, non-nave beagle do

7、gs, andcynomolgus monkeys (three animals per dosing route). Intravenous (IV) administration is dosed via infusionover 30 min in a vehicle containing 5% ethanol, 20% PEG400, and 75% water (pH adjusted to 3.0 with HCl).Oral dosing is administered by gavage in a vehicle containing 5% ethanol, 45% PEG 4

8、00, and 50% of 50 mMcitrate buffer, pH 3. Blood samples are collected over a 24 h period postdose into Vacutainer tubescontaining EDTA-K2. Plasma was isolated, and the concentration of the test compound in plasma wasdetermined with LC/MS/MS after protein precipitation with acetonitrile.MCE has not i

9、ndependently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Proc Natl Acad Sci U S A. 2017 Feb 21;114(8):1922-1927. Int J Radiat Oncol Biol Phys. 2016 Nov 15;96(4):867-876. J Gastroenterol. 2019 Jan 25. Antimicrob Agents Chemother. 2015 Jun;59(6):3482-92. Antimicrob

10、 Agents Chemother. 2015 May;59(5):2496-507.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Link JO, et al. Discovery of ledipasvir (GS-5885): a potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection.J Med Chem. 2014 Mar 13;57(5):2033-46.2. Hernandez D, et al. Natural prevalence of NS5A polymorphisms in subjects infected with hepatitis C virus genotype 3 and their effectson the antiviral activity of NS5A inhibitors. J Clin Virol. 2013 May;57(1):13-8.McePdfHeightCaution: Product has not been