RG7834-RO-7020322-DataSheet-生命科學(xué)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(diǎn): HBV作通路: Anti-infection儲(chǔ)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(shí)驗(yàn) DMSO : 125 mg/mL (311.37 mM; Need ul

2、trasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)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(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適

3、當(dāng)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(qǐng)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(qǐng)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(qǐng)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(xì)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