NVR 3-778

NVR 3-778CAS号: 1445790-55-5分子式: C18H16F4N2O4S分子量: 432.39描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)In vivo(体内研究)

产品描述
描述
NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM belonging to the SBA class It has anti-HBV activity.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:60 mg/mL (138.76 mM)
生物活性
In vitro(体外研究)
NVR 3-778 inhibits the generation of infectious HBV DNA-containing virus particles with a mean antiviral (EC50: 0.40?μM in HepG2.2.15 cells). 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. NVR 3-778 targets HBV core protein and inhibits viral replication. NVR 3-778 has pan-genotypic antiviral activity and a lack of cross-resistance with nucleos(t)ide inhibitors of HBV replication. 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(体内研究)
In dogs following oral administration, NVR 3-778 (1.5?mg/kg; i.g.) shows the mean Cmax and AUC0–inf values of 0.56?μg/ml and 3.50?μg·h/ml, respectively. And the mean oral bioavailability is determined to be 84.6%.