Raltegravir (MK-0518)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Raltegravir，以前称为MK-0518，是一种HIV-1整合酶链转移抑制剂，体外对多耐药性HIV-1和CCR5嗜性及CXCR4嗜性的HIV-1有抑制作用。对这些分子的结构进行修饰，以得到对野生型病毒及选择突变病毒效力最大的的HIV-整合酶抑制剂，并且优化临床前物种中的选择性、药代动力学和代谢特征。Raltegravir源于5,6 –二羟基嘧啶-4-甲酰胺和N-甲基-4-羟基嘧啶酮-甲酰胺的进化。Raltegravir具有强效的抗逆转录病毒作用，10天的单一治疗之后，HIV-1 RNA浓度从基线水平平均减少约2 log10 拷贝每毫升。
参考文献：
Beatriz Grinsztejn, Dr Bach-Yen Nguyen, Christine Katlama, Jose M Gatell, Adriano Lazzarin, Daniel Vittecoq, Charles J Gonzalez, Joshua Chen, Charlotte M Harvey, Robin D Isaacs. Safety and efficacy of the HIV-1 integrase inhibitor raltegravir (MK-0518) in treatment-experienced patients with multidrug-resistant virus: a phase II randomised controlled trial. Then Lancet. 2007. 369(9569): 1261–1269.
Vincenzo Summa, Alessia Petrocchi, Fabio Bonelli, Benedetta Crescenzi, Monica Donghi, Marco Ferrara, Fabrizio Fiore, Cristina Gardelli, Odalys Gonzalez Paz, Daria J. Hazuda, Philip Jones, Olaf Kinzel, Ralph Laufer, Edith Monteagudo, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, Rita Scarpelli, Kara Stillmock, Marc V. Witmer, Michael Rowley. Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection. J. Med. Chem., 2008, 51 (18), pp 5843–5855.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 444.4 |
| Cas No. | 518048-05-0 |
| Formula | C20H21FN6O5 |
| Synonyms | Raltegravir,MK0518 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥19.95 mg/mL in DMSO |
| Chemical Name | N-[2-[4-[(4-fluorophenyl)methylcarbamoyl]-5-hydroxy-1-methyl-6-oxopyrimidin-2-yl]propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=NN=C(O1)C(=O)NC(C)(C)C2=NC(=C(C(=O)N2C)O)C(=O)NCC3=CC=C(C=C3)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
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细胞系 |
MT-4细胞 |
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制备方法 |
在DMSO中的溶解度大于20 mg/mL。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
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反应条件 |
0.0001 ~ 1 μM；5天 |
|
实验结果 |
在低纳摩尔浓度下，Raltegravir抑制SIVmac251复制，其EC50值比对HIV-1 IIIB的EC50值低了约1个数量级。然而，HIV-1比SIVmac251具有更快的细胞致病动力学。抗原捕获ELISA实验结果表明，在人类T细胞系中，Raltegravir对SIVmac251和HIV-1复制具有类似的抑制作用。 |
| 动物实验 [1]: | |
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动物模型 |
感染SIVmac251的恒河猴 |
|
给药剂量 |
100 mg；口服给药；每天2次 |
|
实验结果 |
在感染了SIVmac251的恒河猴中，Raltegravir显著降低病毒负载量，但其作用仅能维持7天。接受Raltegravir治疗的1只恒河猴显示出不可检测的病毒负载量。然而，该恒河猴在治疗开始之前就具有较低的病毒负载量。此外，在非人灵长类动物中，同时给予NRTIs/NtRTIs和Raltegravir稳定地抑制SIVmac251病毒负载量，而对前病毒DNA无效果。 |
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注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
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References: [1]. Lewis MG1, Norelli S, Collins M, Barreca ML, Iraci N, Chirullo B, Yalley-Ogunro J, Greenhouse J, Titti F, Garaci E, Savarino A. Response of a simian immunodeficiency virus (SIVmac251) to raltegravir: a basis for a new treatment for simian AIDS and an animal model for studying lentiviral persistence during antiretroviral therapy. Retrovirology. 2010 Mar 16;7:21. |
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质量控制和MSDS
- 批次:
化学结构
相关生物数据
