Cas No.: | 2072057-17-9 |
Chemical Name: | RG7834 |
SMILES: | CC(C)[C@@H]1CC2=CC(=C(C=C2C3=CC(=O)C(=CN13)C(=O)O)OC)OCCCOC |
Formula: | C22H27NO6 |
M.Wt: | 401.46 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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]. |
Target: | IC50: 2.8 nM (HBsAg), 2.6 nM (HBeAg), 3.2 nM (HBV DNA)[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]. |
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]. |
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. |