RG7834-RO-7020322-DataSheet-生命科學試劑-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作靶點: HBV作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (311.37 mM; Need ul

2、trasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適

3、當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.18 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.18 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的

4、抑制劑師www.MedChemESolubility: 2.08 mg/mL (5.18 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 RG7834 (RO 7020322)種度選擇性、可服的 HBV 抑制劑，在 dHepaRG 細胞中，能夠有效抑制 HBV抗原 HBsAg，HBeAg 和 HBV DNA，IC50 值分別為 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體外研究 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.體內(nèi)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