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.product-side h2 span {width: 50%;}.product-side h2 span.hover {}Related ProductsMK-5172 hydrateAsunaprevir (BMS-650032)Danoprevir (RG7227)SimeprevirMK-5172 potassium saltMK-5172Molarity CalculatorDilution Calculator NarlaprevirHCV NS3 protease inhibitorCatalog No.A3643SizePriceStockQty10mM (in 1mL DMSO)$958.00In stock 10mg$871.00In stock 50mg$1,411.00In stock 100mg$2,465.00In stock Tel: +1-832-696-8203Email: sales@apexbt.comWorldwide Distributors Add to CartBulk InquiryFree samples Check OutSample solution is provided at 25 µL, 10mM.Publications citing ApexBio ProductsNature.2017 Jan 19;541(7637):417-420.Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control Quality Control & MSDS View current batch: 1 Purity = 98.00% COA (Certificate Of Analysis) MSDS (Material Safety Data Sheet) Datasheet Chemical structure Biological ActivityDescriptionNarlaprevir is a potent, selective, orally bioavailable inhibitor of NS3 protease with Ki and EC90 values of 6 nM and 40 nM, respectively.TargetsNS3 proteaseIC50(Ki=6 nM; EC90=40 nM)Narlaprevir Dilution CalculatorConcentration (start)xVolume (start)=Concentration (final)xVolume (final) femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter femtomolar picomolar nanomolar micromolar millimolar molar microliter milliliter liter C1V1C2V2calculateNarlaprevir Molarity CalculatorMass=ConcentrationxVolumexMW* picograms nanograms micrograms milligrams grams kilograms femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter g/molcalculate Chemical Properties Cas No. 865466-24-6SDF Download SDF Synonyms SCH 900518;SCH900518;SCH-900518 Chemical Name (1R,2S,5S)-3-[(2S)-2-[[1-(tert-butylsulfonylmethyl)cyclohexyl]carbamoylamino]-3,3-dimethylbutanoyl]-N-[(3S)-1-(cyclopropylamino)-1,2-dioxoheptan-3-yl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide Canonical SMILES CCCCC(C(=O)C(=O)NC1CC1)NC(=O)C2C3C(C3(C)C)CN2C(=O)C(C(C)(C)C)NC(=O)NC4(CCCCC4)CS(=O)(=O)C(C)(C)C Formula C36H61N5O7S M.Wt 707.96 Solubility Soluble in DMSO Storage Store at -20°CShipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon requestGeneral tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. Background Narlaprevir is a potent and second generation inhibitor of HCV NS3 protease with Ki value of 6 nM [1]. HCV infection is a global problem of public health. It can even cause liver cirrhosis and hepatocellular carcinoma. As an essential enzyme of HCV replication, NS3 serine protease is thought to be an attractive target for HCV infection treatment. Narlaprevir is one of the small inhibitors of NS3 protease. Unlike boceprevir, narlaprevir is a single isoform and shows improved potency. In the inhibiting process of NS3 protease, narlaprevir firstly binds the enzyme with noncovalent interactions and then binds the active-site Ser139 with a reversible covalent bond [1, 2 and 3]. In the in vitro assay, narlaprevir inhibited genotyoes 1a, 1b, 2a and 3a NS3 proteases with Ki values of 0.7, 7, 3 and 7 nM, respectively. In the virus replicon-inhibition assay, narlaprevir showed significant antiviral efficacy with EC50 and EC90 values of 20 and 40 nM, respectively. Besides that, narlaprevir had no cytotoxicity for the host cells. Narlaprevir is also used as a combination therapy with pegylated interferon. The combination treatment of narlaprevir and interferon alfa-2b showed elevated activity in replicon inhibition than the monotherapy of narlaprevir alone [2]. Narlaprevir has improved pharmacokinetic profile of both AUC and bioavailability in animal trials. It showed AUC of 6.5 μM·h, 1.1 μM·h and 0.9 μM·h in rats, monkeys and dogs, respectively. The bioavailabilities of narlaprevir in the three kinds of animals are 46%, 46% and 29%, respectively [1]. Some drug resistant mutations have been identified in the selection with high concentrations of narlaprevir, such as A156T (EC50 value of 1 μM), T54A (EC50 value of 11 nM) and the double mutation (T54A and A156T). Narlaprevir was also found to have cross-resistance to the mutations, such as V170A, F43C and V36M (EC50 value of 8 nM), which are resistant against boceprevir [2, 3].References:[1]. Arasappan A, Bennett F, Bogen S L, et al. Discovery of narlaprevir (SCH 900518): a potent, second generation HCV NS3 serine protease inhibitor. ACS Medicinal Chemistry Letters, 2010, 1(2): 64-69.[2]. Tong X, Arasappan A, Bennett F, et al. Preclinical characterization of the antiviral activity of SCH 900518 (narlaprevir), a novel mechanism-based inhibitor of hepatitis C virus NS3 protease. Antimicrobial agents and chemotherapy, 2010, 54(6): 2365-2370.[3]. Wang H, Geng L, Chen B Z, et al. Computational study on the molecular mechanisms of drug resistance of Narlaprevir due to V36M, R155K, V36M+ R155K, T54A, and A156T mutations of HCV NS3/4A protease. Biochemistry and Cell Biology, 2014, 92(5): 357-369.
APExBIO(APExBIO Technology LLC)总部位于美国休斯顿,是一家自主研发生产、致力于为生命科学研究提供高性能产品和优质服务的供应商。公司现阶段涵盖丰富的产品线,主要包括:1. 10000 多种小分子抑制剂/激动剂——用于肿瘤、免疫、神经等生物医药各研究领域。2. 40 余个高通量化合物库——药物筛选最佳工具。3. 分子生物学产品——PCR、逆转录、qPCR、克隆、高通量 DNA 文库构建等试剂和试剂盒,公司对相关酶进行改造,使其稳定性、催化活性等有极大的提升。4. 体外转录——公司拥有国内独家mRNA体外转录合成平台,提供优质的修饰核苷酸、转录酶等各种合成原料,并可提供mRNA订制服务。5. Cy 染料、生物素——高纯度、种类丰富的 Cy 染料和生物素可用于蛋白检测、纯化等研究。6. 免疫学产品——各类细胞器染料及靶标信号放大的链霉亲和素系列和TSA系列。7. 试剂盒——高性能的 MTT、CCK-8、EdU 细胞增殖与毒性检测 Kit 和 Annexin V、Caspase 凋亡检测 Kit。8. 蛋白研究——蛋白提取抑制剂 cocktail、磷酸化蛋白研究新工具 phosbind。9. 组学服务——提供微生物多样性、转录组学等高通量测序服务。
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