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.product-side h2 span {width: 50%;}.product-side h2 span.hover {}Related ProductsMK-5172 hydrateMK-5172 potassium saltMK-5172 sodium saltTelaprevir (VX-950)MK-5172Danoprevir (RG7227)Molarity CalculatorDilution Calculator Asunaprevir (BMS-650032)NS3 protease inhibitorCatalog No.A3195SizePriceStockQty10mM (in 1mL DMSO)$450.00In stock 5mg$287.00In stock 10mg$484.00In stock 50mg$871.00In stock Tel: +1-832-696-8203Email: sales@apexbt.comWorldwide Distributors Add to CartBulk InquiryFree samples Check OutSample solution is provided at 25 µL, 10mM.Product Citations1. Rago F, DiMare MT, et al. "Degron mediated BRM/SMARCA2 depletion uncovers novel combination partners fortreatment of BRG1/SMARCA4-mutant cancers." Biochem Biophys Res Commun. 2019 Jan 1;508(1):109-116.PMID:305278102. Nadia Hegarat, Adrijana Crncec, et al. "Cyclin A triggers Mitosis either via Greatwall or Cyclin B." bioRxiv. 2018 December 19.Related Compound Libraries DiscoveryProbe™ Bioactive Compound LibraryDiscoveryProbe™ Anti-infection Compound LibraryDiscoveryProbe™ Protease Inhibitor LibraryQuality Control Quality Control & MSDS View current batch: 21 Purity = 99.68% COA (Certificate Of Analysis) HPLC(Retest) MSDS (Material Safety Data Sheet) Datasheet Purity = 99.80% COA (Certificate Of Analysis) HPLC(Retest) NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Chemical structure Related Biological Data Related Biological Data ProtocolKinase experiment [1]:Hepatitis C virus (HCV) NS3/4A protease genotype assaysPublished methods for the construction, expression, and purification of recombinant full-length NS3/4A complexes representing HCV genotypes 1a (H77c) and 1b (J4L6S) were used to generate homogeneous full-length NS3/4A protease complexes representing the six major HCV genotypes (HC-J6, HC-J8, S52, ED43, SA13 and HK-6A). The susceptibility of purified recombinant NS3/4A protease complexes was assessed using fluorescence resonance energy transfer (FRET) assays. The IC50 value was calculated.Cell experiment [1]:Cell linesHuH-7, MRC5, MT-2, HepG2, HeLa and HEK293 cellsPreparation methodSoluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.Reaction Conditions4 daysApplicationsAsunaprevir inhibited HCV RNA replication in different cell lines, including liver, T lymphocytes, lung, cervix, and embryonic kidney. It showed no obvious activity against other RNA viruses.Animal experiment [2]:Animal modelsRatsDosage form10 μM; p.o.; 60 minsApplicationsAfter oral dosing to the rat, Asunaprevir demonstrated modest oral bioavailability and a plasma AUC of 1.0 μM·h. However, at the 24th hrs after p.o. dosing, the liver levels of Asunaprevir were high at 15.2 μM, suggesting a hepatotropic distribution in vivo.Other notesPlease test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.References:[1]. McPhee F, Sheaffer AK, Friborg J, Hernandez D, Falk P, Zhai G, Levine S, Chaniewski S, Yu F, Barry D, Chen C, Lee MS, Mosure K, Sun LQ, Sinz M, Meanwell NA, Colonno RJ, Knipe J, Scola P. Preclinical Profile and Characterization of the Hepatitis C Virus NS3 Protease Inhibitor Asunaprevir (BMS-650032). Antimicrob Agents Chemother. 2012 Oct;56(10):5387-96.[2]. Scola PM, Sun LQ, Wang AX, Chen J, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D"Andrea SV, Zheng B, Hewawasam P, Tu Y, Friborg J, Falk P, Hernandez D, Levine S, Chen C, Yu F, Sheaffer AK, Zhai G, Barry D, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Good AC, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Mueller L, Colonno RJ, Grasela DM, Adams SP, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Meanwell NA, McPhee F. The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection. J Med Chem. 2014 Mar 13;57(5):1730-52.Asunaprevir (BMS-650032) 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 C1V1C2V2calculateAsunaprevir (BMS-650032) 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. 630420-16-5SDF Download SDF Synonyms BMS-650032;BMS 650032;BMS650032,Asunaprevir Chemical Name tert-butyl N-[(2S)-1-[(2S,4R)-4-(7-chloro-4-methoxyisoquinolin-1-yl)oxy-2-[[(1R,2S)-1-(cyclopropylsulfonylcarbamoyl)-2-ethenylcyclopropyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate Canonical SMILES CC(C)(C)C(C(=O)N1CC(CC1C(=O)NC2(CC2C=C)C(=O)NS(=O)(=O)C3CC3)OC4=NC=C(C5=C4C=C(C=C5)Cl)OC)NC(=O)OC(C)(C)C Formula C35H46ClN5O9S M.Wt 748.29 Solubility ≥37.4145 mg/mL in DMSO, ≥48.6 mg/mL in EtOH, Storage Store at -20°CPhysical AppearanceA solidShipping 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. BackgroundAsunaprevir is an orally efficacious inhibitor of NS3 protease with IC50 value of 1nM [1].Asunaprevir is an inhibitor of hepatitis C virus (HCV) NS3 protease. It can inhibit 6 major genotypes of HCV NS3/4A protease with IC50 values of 0.7nM, 0.3nM, 15nM, 78nM, 320nM, 1.6nM, 1.7nM and 0.9nM, respectively for genotype 1a, 1b, 2a, 2b, 3a, 4a, 5a and 6a, respectively. When using the purified recombinant full-length HCV NS3/4A protease complexes, asunaprevir shows the Ki values of 0.4nM and 0.2nM, respectively for genotype 1a and genotype 1b. The mechanism of the inhibition is that the acylsulfonamide of asunaprevir interacts with the catalytic site of NS3 protease in a noncovalent manner. Asunaprevir inhibits HCV RNA replication in different cell lines, including liver, T lymphocytes, lung, cervix, and embryonic kidney. It shows no obvious activity against other RNA viruses. The permeability of asunaprevir is similar to the compound with good absorption in humans. The tests of metabolism rate show that asunaprevir exhibits low to intermediate metabolic clearance. Plasma and tissue exposures in vivo indicate that asunaprevir displays a hepatotropic disposition [2].References:[1] Scola PM, Sun LQ, Wang AX, Chen J, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D"Andrea SV, Zheng B, Hewawasam P, Tu Y, Friborg J, Falk P, Hernandez D, Levine S, Chen C, Yu F, Sheaffer AK, Zhai G, Barry D, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Good AC, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Mueller L, Colonno RJ, Grasela DM, Adams SP, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Meanwell NA, McPhee F. The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection. J Med Chem. 2014 Mar 13;57(5):1730-52. [2] McPhee F, Sheaffer AK, Friborg J, Hernandez D, Falk P, Zhai G, Levine S, Chaniewski S, Yu F, Barry D, Chen C, Lee MS, Mosure K, Sun LQ, Sinz M, Meanwell NA, Colonno RJ, Knipe J, Scola P. Preclinical Profile and Characterization of the Hepatitis C Virus NS3 Protease Inhibitor Asunaprevir (BMS-650032). Antimicrob Agents Chemother. 2012 Oct;56(10):5387-96.
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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