RG7834-RO-7020322-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERG7834Cat. No.: HY-117650ACAS No.: 2072057-17-9Synonyms: RO 7020322分式: CHNO分量: 401.45作靶点: HBV作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (311.37 mM; Need ul

2、trasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4910 mL 12.4549 mL 24.9097 mL5 mM 0.4982 mL 2.4910 mL 4.9819 mL10 mM 0.2491 mL 1.2455 mL 2.4910 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适

3、当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.18 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.18 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的

4、抑制剂师www.MedChemESolubility: 2.08 mg/mL (5.18 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 RG7834 (RO 7020322)种度选择性、可服的 HBV 抑制剂，在 dHepaRG 细胞中，能够有效抑制 HBV抗原 HBsAg，HBeAg 和 HBV DNA，IC50 值分别为 2.8，2.6 和 3.2 nM 1。IC50 & Target IC50: 2.8 nM (HBsAg), 2.6 nM (HBeAg), 3.2 nM (HBV DNA) 1体外研究 RG7834 (S)-(+)-64) is a

5、 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 Cells1.RG7834 has no activity against CYP3A4, CYP2D6, CYP2C9 (IC50s 50 M) or hERG channel 1.体内研究 RG7834 (4 mg/kg, tw

6、ice daily for 21 days) shows anti-HBV efficacy in HBV-infected human liver chimericuPA-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.Animal Model: HBV-infected human liver chimeric uPA-SCID mice 1Dosage: 4 mg/kgAdministration: Twice

7、 daily for 21 daysResult: Reduced both HBsAg and HBeAg, also decreased serum HBV DNA by 0.6 log10 inmice.REFERENCES1. Han X, et al. Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus ExpressionInhibitor with Novel Mechanism of Action. J Med Chem. 2018 Oct 4.McePdfHeightCaution: Product has not been fully validated for medical applications.For research