| Description | RG7834 (RO 7020322) is a highly selective and orally bioavailable inhibitor of HBV(HBsAg and HBeAg and HBV DNA with IC50s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells). |
| In vitro | RG7834 ((S)-(+)-64) 是一种高度选择性且可口服生物利用的HBV抑制剂，抑制HBV抗原（包括HBsAg与HBeAg）及HBV DNA。RG7834 在dHepaRG细胞中其IC50分别为2.8、2.6和3.2 nM。RG7834对CYP3A4、CYP2D6、CYP2C9（IC50s均超过50 μM）或hERG通道无活性。 |
| In vivo | 在HBV感染的人肝嵌合uPA-SCID小鼠中，RG7834表现出抗HBV效力。RG7834（2, 14.5 mg/kg, p.o.）显示出良好的口服生物利用度，并且在小鼠体内具有4.9小时的半衰期。 |
| Target activity | HBV DNA:3.2 nM , HBsAg:2.8 nM , HBeAg:2.6 nM |
| Synonyms | RO 7020322 |
| molecular weight | 401.45 |
| Molecular formula | C22H27NO6 |
| CAS | 2072057-17-9 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (311.37 mM), Sonication is recommended. |
| References | 1. Han X, et al. Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action. J Med Chem. 2018 Oct 4. |