奧比他韋作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetOmbitasvirCat. No.: HY-13997CAS No.: 1258226-87-7分式: CHNO分量: 894.11作靶點(diǎn): HCV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 : 33 mg/mL (36.91 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)

2、備液1 mM 1.1184 mL 5.5922 mL 11.1843 mL5 mM 0.2237 mL 1.1184 mL 2.2369 mL10 mM 0.1118 mL 0.5592 mL 1.1184 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；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。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)娜芙獍浮Ｒ韵氯芙獍付颊?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶

3、劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.80 mM); Clear solution此案可獲得 2.5 mg/mL (2.80 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 4

4、00 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.80 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (2.80 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL

5、ACTIVITY物活性 Ombitasvir種 HCV NS5A 抑制劑，對(duì) HCV基因型 1-5 和 6a 的 EC50 值分別為 0.82-19.3 pM 和 366 pM。IC & Target EC50: 0.82 to 19.3 pM (HCV genotypes 1 to 5), 366 pM (HCV genotype 6a)1體外研究 Ombitasvir is active against the genotype 2a JFH-1 replicon, with an EC50 of 0.82 pM, and the EC50s of ombitasvir are42 pM

6、and 68 pM against the L28 and F28 variants of this genotype 6a replicon, respectively1. In GT1a, variantsM28V, L31V, and H58D confers 58- to 243-fold resistance to Ombitasvir. Single variants M28T, Q30R, and Y93C/Sconfers 800- to 8965-fold resistance, while Y93H/N confers 40000-fold resistance to Om

7、bitasvir2.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Virol. 2018 Jan 2;92(2). pii: e01582-17. Antiviral Res. 2017 Mar;139:18-24. Chem Cent J. 2017 Jan 3;11:1. Xenobiotica. 2018 Nov 8:1-10. J Liq ChromaTogr R T. 2019 Mar.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Krishnan P, et al. In vitro

8、and in vivo antiviral activity and resistance profile of ombitasvir, an inhibitor of hepatitis C virus NS5A. Antimicrob AgentsChemother. 2015 Feb;59(2):979-872. DeGoey DA, et al. Discovery of ABT-267, a pan-genotypic inhibitor of HCV NS5A. J Med Chem. 2014 Mar 13;57(5):2047-57McePdfHeightCaution: Product has not been fully validated for medical applications. For research use on