- Anguizole
- Asunaprevir (BMS-650032)
- Balapiravir
- BMS-790052 dihydrochloride
| LedipasvirHCV NS5A protein 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.
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- Purity = 99.21%
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Chemical structure
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| Cas No. | 1256388-51-8 | SDF | Download SDF |
| Synonyms | GS-5885;GS 5885;GS5885 | ||
| Chemical Name | GS-5885;GS 5885;GS5885 | ||
| Canonical SMILES | CC([C@@](/N=C(OC)O)([H])C(N1CC2(C[C@@]1([H])C3=NC=C(N3)C4=CC5=C(C6=C(C5(F)F)C=C(C7=CC(N8)=C(N=C8[C@]9([H])[C@@]%10([H])CC[C@](N9C([C@](/N=C(OC)O)([H])C(C)C)=O)([H])C%10)C=C7)C=C6)C=C4)CC2)=O)C | ||
| Formula | C49H54F2N8O6 | M.Wt | 889 |
| Solubility | ≥44.45 mg/mL in DMSO, ≥46.9 mg/mL in EtOH with gentle warming, <2.52 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. | ||
Ledipasvir is an inhibitor of the hepatitis C virus replication with IC50 value of 141 nM [1].
Hepatitis C virus (HCV) is an enveloped (+)-single stranded RNA virus, which is the cause of hepatitis C and some cancer lymphomas. The viral RNA is replicated in host cell via RNA-dependent RNA polymerase of HIV and then assembled into virions. The zinc-binding phosphoprotein NS5A protein is translated from HCV genome, which plays important role in the virus replication process. It may act as an transcriptional activator for NS5A RNA replication system and also the mediator of virion assembly.
Ledipasvir is a specific inhibitor of HCV NS5A protein to inhibit HCV replication in the HCV subgenomic replicon system. NS5A replication complex inhibitors are novel antiviral factors for HCV treatment. Typically, these inhibitors have high efficiency and low viral resistance when compared to traditional HCV replication inhibitor targeted on NS3 helicase and NS5B RNA polymerasae. NS5A inhibitors are supposed to bind across the NS5A dimer interface, proximal to N-terminal domain 1. The binding is thought to distort dimer association directly or allosterically, which may disrupt NS5A function in HCV RNA replication [2]. When a JFH1/3a-NS5A hybrid replicon was used to assess susceptibility to NS5A, another inhibitor DCV was shown to be more potent than ledipasvir. Additionally, NS5A-A30K and -Y93H variants exhibited reduced sensitivity to ledpasvir (EC50 value of 1770 nM and 4300 nM respectively) [1].
In clinical trials, it was observed ledpasvir was well tolerated and exhibited median maximal reduction of HCV RNA ranging from 2.3 log10 IU/ml to 3.3 log10 IU/ml. Emax modeling also showed administration of 30 mg ledpasvir after 3 days resulted in >95% maximal response of HCV RNA reduction to genotype 1a.Finally, it was also observed that HCV RNA was more sustained in genotype 1b compared to 1a [3].
References:[1] Hernandez D et al. , Natural prevalence of NS5A polymorphisms in subjects infected with hepatitis C virus genotype 3 and their effects on the antiviral activity of NS5A inhibitors. J Clin Virol. 2013, 57(1): 13-8.[2] Gao M et al. , Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect. Nature. 2010, 465: 96-100.[3] Lawitz E J et al. , A phase 1, randomized, placebo-controlled, 3-day, dose-ranging study of GS-5885, an NS5A inhibitor, in patients with genotype 1 hepatitis C. J Hepatol. 2012, 57(1): 24-31.
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核酸是天然高分子化合物，，糖类中的多糖（淀粉、纤维素、糖原等）也是天然高分子化合物
同属于生命的六大营养物质（水，无机盐，糖类，脂质，核酸，蛋白质）
1.CA15-3属于多形上皮黏蛋白。CA15-3测定广泛用于乳腺癌的辅助诊断。60%～80％进展期乳腺癌患者的CA15-3浓度大30kU/L。CA15-3有助于判断肿瘤的进展和疗效，测定值大于1000kU/L者预后不良。在乳腺癌初期其灵敏度较低，在Ⅲ期时约为12%，因此CA15-3测定不能用作乳腺癌的筛选手段．当怀疑乳腺癌而CA15-3又正常时，可以结合CEA值进行考虑。应注意到治疗后由于肿瘤细胞死亡，CA15-3起初会升高，然后才逐渐下降。持续不降或上升者则提示病情恶化。
2．其他恶性肿瘤，如肺、结肠、胰腺、肝脏、卵巢癌、子宫颈和子宫内膜的恶性肿瘤也都可见到CA15-3不同程度的阳性率（低于10%）。
3．肝硬化、肝炎、结节病、结核病、自身免疫性疾病（SLE)以及卵巢、乳腺的良性病变中，CA15-3值略高于正常范围，但阳性率一般低于10%，妊娠中后期，有近一半孕妇血清CA15-3升高。
还有如果用气相做糖的鉴别的话，需要样品量大不大？怎么衍生化？
不好意思，我是学药分的，对植化比较外行，请详细些，谢了先！
一般情况下同时测定蔗糖、果糖和葡萄糖。
选用哪种检测器呐。
本来经战友的意见已决定用示差了，但突然有个经销商愿意以比较优惠的价格卖蒸发光给我们，所以又开始犹豫了。
最后一次请教各位战友，如题目。谢谢！！
