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编 号:F165670
分子式:C18H16F4N2O4S
分子量:432.39
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity.

体内研究:
NVR 3-778 (1.5?mg/kg; i.g.) displays the mean Cmax and AUC0–inf values of 0.56?μg/ml and 3.50?μg·h/ml, respectively, in dogs following oral administration. And the mean oral bioavailability is determined to be 84.6%.Animal Model:Dogs
Dosage:1.5?mg/kg (Pharmacokinetic Analysis)
Administration:Oral gavage
Result:The mean Cmax and AUC0–inf values are 0.56?μg/ml and 3.50?μg·h/ml and the oral bioavailability is 84.6%.

体外研究:
NVR 3-778 targets HBV core protein and inhibits viral replication.NVR 3-778 inhibits the generation of infectious HBV DNA-containing virus particles with a mean antiviral with an EC50 of 0.40?μM in HepG2.2.15 cells.NVR 3-778 exhibits pan-genotypic antiviral activity and a lack of cross-resistance with nucleos(t)ide inhibitors of HBV replication.NVR 3-778 inhibits pregenomic RNA encapsidation, viral replication, and the production of HBV DNA- and HBV RNA-containing particles. NVR 3-778 also inhibits de novo infection and viral replication in primary human hepatocytes with EC50s of 0.81?μM against HBV DNA and between 3.7μM and 4.8?μM against the production of HBV antigens and intracellular HBV RNA.The EC50 values of NVR 3-778 are increased by 4.5-, 9.3-, and 15.8-fold in the presence of 10%, 20%, and 40% human serum, respectively.
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