- R-7128
- VCH-916
- T 705
| NesbuvirNS5B polymerase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.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 & MSDS
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- Purity = 99.79%
- COA (Certificate Of Analysis)
- HPLC (Retest)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | Nesbuvir is a selective inhibitor of HCV NS5B RNA-dependent RNA polymerase. | |||||
| Targets | HCV NS5B RNA-dependent RNA polymerase | |||||
| IC50 | ||||||
| Cell experiment[1]: | |
Cell lines | Huh7-BB7 cells |
Preparation method | The solubility of this compound in DMSO is > 22.3 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 condition | 7 d, 40-80 nM |
Applications | Nesbuvir is an inhibitor of the hepatitis C virus （HCV）nonstructural protein 5B (NS5B) polymerase. It has potent and specific inhibitory effect against the HCV RdRp, thus inhibiting RNA synthesis. When Nesbuvir is used in combination with boceprevir, it decreases the frequency with which resistant variants occur in Huh7-BB7 cells bearing a subgenomic genotype 1b HCV replicon. |
| Animal experiment [2]: | |
Animal models | Urokinase plasminogen activator (uPA)/severe combined immunodeficient (SCID) mice |
Dosage form | Oral administration, 50 mg/kg，three times daily for 5 days |
Application | Treating mice with Nesbuvir resulted in a 2.02 ± 0.55 log10 decrease of HCV titer with one mouse below the level of detection, whereas HCV levels in the control group of mice were relatively stable (0.26 ± 0.16 log10 decline). |
Other notes | Please 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]. Flint M, Mullen S, Deatly A M, et al. Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034)[J]. Antimicrobial agents and chemotherapy, 2009, 53(2): 401-411. [2]. Kneteman N M, Howe A Y M, Gao T, et al. HCV796: a selective nonstructural protein 5B polymerase inhibitor with potent anti‐hepatitis C virus activity in vitro, in mice with chimeric human livers, and in humans infected with hepatitis C virus[J]. Hepatology, 2009, 49(3): 745-752. | |
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| Cas No. | 691852-58-1 | SDF | Download SDF |
| Synonyms | HCV 796;HCV-796;HCV796,Nesbuvir | ||
| Chemical Name | 5-cyclopropyl-2-(4-fluorophenyl)-6-[2-hydroxyethyl(methylsulfonyl)amino]-N-methyl-1-benzofuran-3-carboxamide | ||
| Canonical SMILES | CNC(=O)C1=C(OC2=CC(=C(C=C21)C3CC3)N(CCO)S(=O)(=O)C)C4=CC=C(C=C4)F | ||
| Formula | C22H23FN2O5S | M.Wt | 446.49 |
| Solubility | ≥22.3 mg/mL in DMSO, ≥97.8 mg/mL in EtOH with gentle warming, <2.59 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For 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. | ||
Nesbuvir is a novel selective inhibitor of nonstructural protein 5B (NS5B) polymerase with IC50 value of 5 nM [1].
NS5B (nonstructural protein 5B) is a viral protein found in HCV and plays an important role in HCV RNA replicate by using the viral positive RNA strand as its template and catalyzing the polymerization of rNTP during RNA replication. As the principal catalytic enzyme for HCV replication, NS5B is a viable target for HCV-RNA replication and used as a target for HCV therapy [2] [3].
Nesbuvir is a selective NS5B polymerase inhibitor and has a different selectivity with the reported ALK inhibitor crizotinib. When tested with Huh7.5 cell line, nesbuvir showed the highest selectivity for NS5B and mutations reduced the cells susceptibility [1]. In Clone A cells derived from Huh-7 cells containing approximately 1,000 genome copies of HCV genotype 1b replicon per cell, nesbuvir treatment with the concentration of 0.1 and 1 μM for 16-day reduced about 3.6 log10 and 4.2 log10 HCV RNA levels, respectively [2].
In the chimeric mouse model, nesbuvir treatment resulted in a 2.02 +/- 0.55 log reduction in HCV titer, whereas in combination with interferon using a suboptimal dose of 30 mg/kg three times per day showed a 2.44 log reduction and were better than interferon treatment only [4].
References: [1]. Flint, M., et al., Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034). Antimicrob Agents Chemother, 2009. 53(2): p. 401-11.[2]. Howe, A.Y., et al., Molecular mechanism of hepatitis C virus replicon variants with reduced susceptibility to a benzofuran inhibitor, HCV-796. Antimicrob Agents Chemother, 2008. 52(9): p. 3327-38.[3]. Meshram, R.J. and R.N. Gacche, Effective epitope identification employing phylogenetic, mutational variability, sequence entropy, and correlated mutation analysis targeting NS5B protein of hepatitis C virus: from bioinformatics to therapeutics. J Mol Recognit, 2015.[4]. Kneteman, N.M., et al., HCV796: A selective nonstructural protein 5B polymerase inhibitor with potent anti-hepatitis C virus activity in vitro, in mice with chimeric human livers, and in humans infected with hepatitis C virus. Hepatology, 2009. 49(3): p. 745-52.
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感觉这样的提问是没有意义的
还是自己找下资料吧
求助大家，小分子药物最新专利申请情况跟踪，之前听别人说可以在一个网站可以导出这个信息。
不知哪位大侠知道，告知一下，不胜感激！
脂质的生物学功能有1、脂肪氧化分解释放能量
2、复合脂质和衍生脂质是构成细胞的成分
3、促进脂性维生素的吸收
4、脂肪防震和隔热保温作用
5、脂肪的氧化利用具有降低蛋白质和糖消耗的作用
有机的是有机化合物的简称,它指的是含碳化合物.
但是,有四大类常见物质一般不作为有机物处理：
1、碳的氧化物,如CO和CO2.
2、碳酸及其盐,如CaCO3.
3、金属碳化物,如CaC2.
4、拟卤素及其化合物,如(CN)2与KSCN.
水的化学式为H2O,它不含有碳元素,故不是有机物.
但若所描述的水不是化学意义的水,而是自然界存在的天然水,那么,水中会溶有一定量的有机物.
从交联剂的配制，以及交联反应体系，交联后样品是否沸水煮10min,最后SDS-PAGE检测。
