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RG7834

Names

[ CAS No. ]:
2072057-17-9

[ Name ]:
RG7834

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Anti-infection >> HBV

[Target]

IC50: 2.8 nM (HBsAg), 2.6 nM (HBeAg), 3.2 nM (HBV DNA)[1]


[In Vitro]

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].

[In Vivo]

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].

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H27NO6

[ Molecular Weight ]:
401.45

[ Storage condition ]:
2-8℃


Related Compounds

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