NVR 3-778

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NVR 3-778 (NVR3-778、NVR 3778) 是一种 HBV 复制的小分子抑制剂，靶向病毒核心蛋白，这是一种一流的衣壳组装调节剂。

NVR 3-778 (NVR3-778, NVR 3778) is a small molecule inhibitor of HBV replication that targets the viral core protein, a first-in-class capsid assembly modulator; inhibits the generation of infectious HBV DNA containing virus particles with EC50 of 0.40 uM in HepG2.2.15 cells; NVR 3-778 inhibits pgRNA encapsidation, viral replication and the production of HBV DNA- and HBV RNA-containing particles, also inhibits de novo infection and viral replication in primary human hepatocytes with EC50 of 0.81 uM against HBV DNA and 3.7-4.8 uM against the production of HBV antigens and intracellular HBV RNA; demonstrates favorable pharmacokinetics and safety in animal species.HBV Infection Phase 1 Clinical(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 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%.

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.

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%.

NVR3-778 | NVR 3778

Microbiology/Virology

HBV

HBV

Infection

HBV Infection

1445790-55-5

432.39

C18H16F4N2O4S

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (578.18 mM)

O=C(NC1=CC(F)=C(F)C(F)=C1)C2=CC=C(F)C(S(=O)(N3CCC(O)CC3)=O)=C2

4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide

(-20℃)

With Ice Pack

≥ 2 years