JNJ-678-JNJ-53718678-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEJNJ-678Cat. No.: HY-112180CAS No.: 1383450-81-4Synonyms: JNJ-53718678分式: CHClFNOS分量: 500.92作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 65 mg/mL (129.76 mM; Need ul

2、trasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.17 mg/mL (4.33 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.17 mg/mL (4.33 mM); Suspended solution; Need ultrasonic1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSo

3、lubility: 2.17 mg/mL (4.33 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 JNJ-678 (JNJ-53718678)新型融合蛋 (fusion protein) 抑制剂，临床试验中于治疗呼吸道合胞病毒 (RSV)。IC50 & Target Fusion protein 1体外研究 JNJ-678 (JNJ-53718678) is a small-molecule respiratory syncytial virus (RSV) fusion inhibitor currently underclinical evaluat

4、ion in infants hospitalized for RSV infection. JNJ-678 (JNJ-53718678) binds to RSV F proteinin its prefusion conformation. JNJ-678 (JNJ-53718678) displays very potent antiviral activity and lowcytotoxicity. In addition to its activity against the RSV A2 strain, JNJ-678 (JNJ-53718678) is also highly

5、activeagainst a number of RSV strains from both A and B subtypes. The EC50 in an RSV infection assay usingHeLa cells is 460pM 1.体内研究 Oral treatment of neonatal lambs with JNJ-678 (JNJ-53718678), or with an equally active close analog,efficiently inhibits established acute lower respiratory tract inf

6、ection in the animals, even when treatment isdelayed until external signs of respiratory syncytial virus illness have become visible 1.PROTOCOLCell Assay 1 The antiviral activity of JNJ-678 (JNJ-53718678) against hMPV is evaluated using a cellular infectious assayin 96-well plates in which Vero/TMPR

7、SS2 cells are infected with recombinant hMPV65. Cells are treated withdifferent concentrations of JNJ-678 (JNJ-53718678) and then infected with recombinant hMPV (1104 PFUper well). Three days post-virus exposure, viral replication is quantified by measuring fluorescence and theEC50 is calculated 1.M

8、CE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 1Administration 1 Cotton rats receive either a single dose at 24h after viral infection or once-daily doses of 40mg/kg JNJ-678(JNJ-53718678) by oral gavage, at 24, 48, and 72h after viral infect

9、ion. The decrease of viral replication in allexperiments is compared to challenged animals that received only the vehicle 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Roymans D, et al. Therapeutic efficacy of a respiratory syncytial virus fusion inhibitor. Nat Commun. 2017 Aug 1;8(1):167.McePdfHeightCaution: Product has not been fully validated for me