RG7834 (RO 7020322) (RO 7020322) 是一种高选择性和口服生物可利用的 HBV 抑制剂，有效抑制 HBV 抗原（HBsAg 和 HBeAg）和 HBV DNA，在 dHepaRG 细胞中的 IC50 值分别为 2.8、2.6 和 3.2 nM。
RG7834 (RO 7020322) is a highly selective and orally bioavailable HBV inhibitor, potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC50s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells[1].
RG7834 ((S)-(+)-64) is a highly selective and orally bioavailable HBV inhibitor, potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC50s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells[1].RG7834 has no activity against CYP3A4, CYP2D6, CYP2C9 (IC50s >50 μM) or hERG channel[1].
RG7834 (4 mg/kg, twice daily for 21 days) shows anti-HBV efficacy in HBV-infected human liver chimeric uPA-SCID mice[1].RG7834 (2, 14.5 mg/kg, p.o.) exhibits good oral bioavail ability, with a half-life of 4.9 h in mice[1].
[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.
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