- MK-5172 hydrate
- Asunaprevir (BMS-650032)
- Danoprevir (RG7227)
- Simeprevir
- MK-5172 potassium salt
- MK-5172
| NarlaprevirHCV NS3 protease 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
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | Narlaprevir is a potent, selective, orally bioavailable inhibitor of NS3 protease with Ki and EC90 values of 6 nM and 40 nM, respectively. | |||||
| Targets | NS3 protease | |||||
| IC50 | (Ki=6 nM; EC90=40 nM) | |||||
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| Cas No. | 865466-24-6 | SDF | 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°C |
| 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. | ||
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.
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请教大家一个问题，不同厂家cIEF的Marker能混合使用吗？另外，如果我对其它厂家pI值为6.0的marker进行cIEF测定，那测得的pI值会等于6.0吗？谢谢！
做western时，看着膜上的Marker条带是直的，但是最后显影出来的目的蛋白的条带全部是歪的，这是为什么？两块胶都是这个问题，欲哭无泪呀！！！求高人指点一下，是什么操作不当导致的
已经重复做了4次了，还是曝出9条带。请求各位大神解析解析==
想看下人肿瘤组织内巨噬细胞的浸润情况，我以为一个CD11b就够了。咨询了一下抗体公司，竟然让我订三个抗体，分别是CD11b，CD68和CD163，后两者不是M1和M2的分型吗？
另外查了下CD11b也确实在别的一些免疫细胞有所表达，请教下，有专门的特异性抗体吗？没课题没经费，只能省省省了
英 [?mɑ:k?(r)] 美 [?mɑ:rk?(r)]n.标识，标记； 记号笔，阅卷人； 防守队员； 特征复数： markers
双语例句
Draw your child's outline with a heavy black marker.用浓黑色的毡笔画出你孩子的轮廓。2. He put a marker in his book and followed her out.
他在书里夹了一个书签后便随她出去了。
3. He placed a marker where the ball had landed.他在球落地的地方放了个标记。
4. Step off twenty feet and then place a marker in the ground.先步测20英尺,再在地上做出标记.
5. Step out ten feet and then put a marker in the ground.步测十英尺,然后在地上做出标记.
英 [ˈmɑ:kə(r)] 美 [ˈmɑ:rkə(r)]
n.标识，标记； 记号笔，阅卷人； 防守队员； 特征
复数： markers
双语例句
1. Draw your child's outline with a heavy black marker.
用浓黑色的毡笔画出你孩子的轮廓。
2. He put a marker in his book and followed her out.
他在书里夹了一个书签后便随她出去了。
3. He placed a marker where the ball had landed.
他在球落地的地方放了个标记。
4. Step off twenty feet and then place a marker in the ground.
先步测20英尺,再在地上做出标记.
5. Step out ten feet and then put a marker in the ground.
步测十英尺,然后在地上做出标记.
连续三次都这样，Marker的泳道的位置有很多亮条带，但Marker本来的条带是不亮的。我做了内参和目的，一张胶上左右两部分分别都加样品和Marker，切开转膜分别孵育，一块儿显影，内参的Marker就不会亮，只有目的那一张Marker会亮，昨天做的借了别人的Marker，显影出来还是有那个条带。
我的目的条带还没有Marker那部分的条带亮，Marker的部分非常亮。
