Pibrentasvir-ABT-530-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPibrentasvirCat. No.: HY-101662CAS No.: 1353900-92-1Synonyms: ABT-530分式: CHFNO分量: 1113.18作靶點: HCV作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 62 mg/mL (55.70 mM; Need

2、ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 0.8983 mL 4.4916 mL 8.9833 mL5 mM 0.1797 mL 0.8983 mL 1.7967 mL10 mM 0.0898 mL 0.4492 mL 0.8983 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲

3、備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.25 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (2.25 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Mol

4、ecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (2.25 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pibrentasvir種新型的泛 因型丙型肝炎病毒 (HCV) NS5A 抑制劑，對來 因型 1 6 含有 NS5A 的HCV 復制的 EC50 范 為 1.4 5.0 pM。IC50 & Target HCV 1體外研究 Pibrentasvir inhibits HCV genotype 1a-H77, 1b-Con1, and 2a-JFH-1 subgenomic replicons with

5、50%effective concentrations (EC50s) of 1.8, 4.3, and 5.0 pM, respectively. The antiviral activity of Pibrentasvir isattenuated 35- to 47-fold in the presence of 40% human plasma through sequestration of compound due toplasma protein binding. Pibrentasvir retains full activity against all of the geno

6、type 1a and 1b single-positionNS5A substitutions tested, except Y93H and Y93N in genotype 1a, which confers a 7-fold increase in EC50to Pibrentasvir 1.PROTOCOLCell Assay 1 The inhibitory effect of Pibrentasvir on HCV replication in replicon cells is determined in Dulbeccos modifiedEagles medium (DME

7、M) containing 5% fetal bovine serum with or without 40% human plasma. The cells areincubated with Pibrentasvir for 3 days and are subsequently lysed and processed according to themanufacturers instructions to measure luciferase reporter activity using a Victor II luminometer. The 50%effective concen

8、tration (EC50) value is calculated using nonlinear regression curve fitting to the four-parameter logistic equation in software 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ng TI, et al. In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS5A Inhibitor Pibrentasvir.Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02558-16.McePdfHeightCaution: Product has not been fully validated for medical appli