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.product-side h2 span {width: 50%;}.product-side h2 span.hover {}Related ProductsAnguizoleAsunaprevir (BMS-650032)BalapiravirBMS-790052 dihydrochlorideMolarity CalculatorDilution Calculator Daclatasvir (BMS-790052)HCV NS5A inhibitorCatalog No.A5618SizePriceStockQty10mM (in 1mL DMSO)$180.00In stock 5mg$120.00In stock 25mg$360.00In stock 100mg$980.00In 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.Related Compound Libraries DiscoveryProbe™ FDA-approved Drug LibraryDiscoveryProbe™ Bioactive Compound LibraryDiscoveryProbe™ Anti-infection Compound LibraryDiscoveryProbe™ Protease Inhibitor LibraryQuality Control Quality Control & MSDS View current batch: 1 Purity = 98.00% COA (Certificate Of Analysis) MSDS (Material Safety Data Sheet) Datasheet Chemical structure Biological ActivityDescriptionDaclatasvir (BMS-790052; EBP 883) is a first-in-class, highly-selective oral inhibitor of HCV NS5A with EC50 values of 9-50 pM.TargetsHCV NS5AIC509 pM-50 pM(EC50)ProtocolCell experiment [1]:Cell linesHCV genotypes and the JFH-1 genotype 2a infectious virus in cell culturePreparation methodThe solubility of this compound in DMSO is > 36.6 mg/mL. 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.Reacting conditionEC50: 9 to 146 pMApplicationsBMS-790052 exhibited picomolar half-maximum effective concentrationstowards replicons expressing a broad range of HCV genotypes and the JFH-1 genotype 2a infectious virus in cell culture, with EC50 values ranging from 9 to 146 pM. BMS-790052 displayed similar potency in Huh-7, HeLa and HEK293T cells.Animal experiment [1]:Animal modelspatients chronically infected with HCVDosage formOral administration, 10-100 mgApplicationBMS-790052 was safe and well tolerated in HCV-infected subjects after single oral doses up to 100 mg. In HCV-infected subjects, BMS-790052 had a mean plasma elimination half-life ranging from 10 to 14 h. Administration of a single 100-mg dose of BMS-790052 was associated with a 3.3log 10 reduction in mean viral load measured 24h post-dose that was sustained for an additional 120h in two patients infected with genotype 1b virus.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]. Gao M, Nettles R E, Belema M, et al. Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect[J]. Nature, 2010, 465(7294): 96.Daclatasvir (BMS-790052) 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 C1V1C2V2calculateDaclatasvir (BMS-790052) 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. 1009119-64-5; 1214735-16-6SDF Download SDF Chemical Name methyl N-[(2S)-1-[(2S)-2-[5-[4-[4-[2-[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]phenyl]phenyl]-1H-imidazol-2-yl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamate Canonical SMILES CC(C)C(C(=O)N1CCCC1C2=NC=C(N2)C3=CC=C(C=C3)C4=CC=C(C=C4)C5=CN=C(N5)C6CCCN6C(=O)C(C(C)C)NC(=O)OC)NC(=O)OC Formula C40H50N8O6 M.Wt 738.88 Solubility ≥36.6mg/mL in DMSO Storage Store at -20°C Physical 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. BackgroundDaclatasvir, formerly known as BMS-790052, is a potent NS5A inhibitor with EC50 values varying from 9 to 146 pM. [1,2]The nonstructural 5A (NS5A) is a target in HCV drug development, which is a 447 amino-acid, zinc-binding phosphoprotein who plays an essential but enigmatic role in the virus life cycle. However the function of NS5A has no enzymatic activities, which makes it very difficult to understand the antiviral function of daclatasvir. It is assumed that Daclatasvir may interfere with the dimeric structure of NS5A, effecting subtle structural distortions that interfere with protein function in a specific way.[1,2]The antiviral activity of daclatasvir towards genotypes was assessed by using replication-competent 1a or 1b replicons to construct hybrids in which the entire NS5A coding region or the first 100 amino acids of NS5A from different genotypes replaced the corresponding sequence of the parent replicon. Daclatasvir was reported to be highly potent across all HCV genotypes with half-maximum effective concentrations (EC50) ranging from 9 to 146 pM.[2]A phase I clinical study showed Daclatasvir’s inhibition for HCV viruses. A 1 mg dose of daclatasvir produced a mean 1.8 log10 reduction in serum HCV RNA 24 h after administration. The 10 and 100 mg doses produced 3.2 log10 and 3.3 log10 reductions, respectively. Data collected from clinical trials on daclatasvir illustrated an initial, rapid viral decline followed by a slower fall in HCV RNA, which indicated that by inhibiting NS5A, daclatasvir blocks intracellular HCV RNA synthesis and virion assembly and secretion.[1]References: 1.Herbst D A, Reddy K R. NS5A inhibitor, daclatasvir, for the treatment of chronic hepatitis C virus infection[J]. Expert opinion on investigational drugs, 2013, 22(10): 1337-1346.2.Gao M, Nettles R E, Belema M, et al. Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect[J]. Nature, 2010, 465(7294): 96-100.
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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