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NVR 3-778

CAS No. : 1445790-55-5

產(chǎn)品活性：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.

研究領(lǐng)域：Anti-infection

作用靶點(diǎn)：HBV

In Vitro: 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.

In Vivo: NVR 3-778 (1.5?mg/kg; i.g.) displays the mean C_max and AUC_0–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%.

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