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Raltegravir

产品编号 T2239L CAS 518048-05-0

别名: 雷特格韦, MK-0518

Raltegravir (MK-0518) 是一种HIV 整合酶抑制剂。

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Raltegravir, CAS 518048-05-0

规格	价格/CNY	货期
1 mg	￥ 262	现货
2 mg	￥ 369	现货
5 mg	￥ 567	现货
10 mg	￥ 937	现货
25 mg	￥ 1,720	现货
50 mg	￥ 2,890	现货
100 mg	￥ 4,220	现货
1 mL * 10 mM (in DMSO)	￥ 638	现货

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其他形式的 Raltegravir:

Raltegravir potassium
现货
Raltegravir sodium
询价

选择批次

纯度: 99.77%

纯度: 99.05%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Raltegravir (MK-0518) is a pyrrolidinone derivative and HIV INTEGRASE INHIBITOR that is used in combination with other ANTI-HIV AGENTS for the treatment of HIV INFECTION.
靶点活性	Integrase (S217Q PFV):40 nM, Integrase (WT PFV):90 nM
体外活性	Raltegravir诱导非人灵长类病毒的免疫学改善,并伴有进展性SIVmac251感染.
体内活性	Raltegravir在体外作用于人类T淋巴细胞培养物,有效作用于HIV-1,抑制达95%时浓度为31±20 nM。S217Q PFV IN对Raltegravir的敏感性至少与WT酶相似。在急性感染的人类淋巴CD4 + T细胞系MT-4和CEMx174中,Raltegravir高效抑制SIVmac251复制,EC90处于低纳摩尔范围。Raltegravir微弱抑制肝细胞色素P450。Raltegravir不会诱导CYP3A4 RNA表达或CYP3A4依赖的睾丸激素6-β-羟化酶活性。Raltegravir在镁和钙存在时,细胞扩散性降低。Raltegravir和相关的HIV-1整合酶链转移抑制剂高效阻断病毒复制。
激酶实验	PFV integration assay: For quantitative strand transfer assays, donor DNA substrate is formed by annealing HPLC grade oligonucleotides 5′-GACTCACTATAGGGCACGCGTCAAAATTCCATGACA and 5′-ATTGTCATG GAATTTTGACGCGTGCCCTATAGTGAGTC. Reactions (40 μL) contains 0.75 μM PFV IN, 0.75 μM donor DNA, 4 nM (300 ng) supercoiled pGEM9-Zf(?) target DNA, 125 mM NaCl, 5 mM MgSO4, 4 μM ZnCl2, 10 mM DTT, 0.8% (vol/vol) DMSO, and 25 mM BisTris propane–HCl, pH 7.45. Raltegravir is added at indicated concentrations. Reactions are initiated by addition of 2 μL PFV IN diluted in 150 mM NaCl, 2 mM DTT, and 10 mM Tris-HCl, pH 7.4, and stopped after 1 hour at 37 °C by addition of 25 mM EDTA and 0.5% (wt/vol) SDS. Reaction products, deproteinized by digestion with 20 μg proteinase K for 30 minutes at 37 °C followed by ethanol precipitation, are separated in 1.5% agarose gels and visualized by staining with ethidium bromide. Integration products are quantified by quantitative real-time PCR, using Platinum SYBR Green qPCR SuperMix and three primers: 5′-CTACTTACTCTAGCTTCCCGGCAAC, 5′-TTCGCCAGTTAATAGTTTGCGCAAC, and 5′-GACTCACTATAGGGCACGCGT. PCR reactions (20 μL) contained 0.5 μM of each primer and 1 μL diluted integration reaction product. Following a 5-min denaturation step at 95 °C, 35 cycles are carried out in a CFX96 PCR instrument, using 10 seconds denaturation at 95 °C, 30 seconds annealing at 56 °C and 1 minutes extension at 68 °C. Standard curves are generated using serial dilutions of WT PFV IN reaction in the absence of INSTI.
细胞实验	Human MT-4 cells are infected for 2 hours with the SIVmac251, HIV-1 (IIIB) and HIV-2 (CDC 77618) stocks at a multiplicity of infection of, approximately, 0.1. Cells are then washed three times in phosphate buffered saline, and suspended at 5 × 105/mL in fresh culture medium (to primary cells 50 units/mL of IL-2 are added) in 96-well plates, in the presence or absence of a range of triplicate raltegravir concentrations (0.0001 μM -1 μM). Untreated infected and mock-infected controls are prepared too, in order to allow comparison of the data derived from the different treatments. Viral cytopathogeniciy in MT-4 cells is quantitated by the methyl tetrazolium (MTT) method (MT-4/MTT assay) when extensive cell death in control virus-infected cell cultures is detectable microscopically as lack of capacity to re-cluster. The capability of MT-4 cells to form clusters after infection. Briefly, clusters are disrupted by pipetting; and, after 2 hours of incubation at 37 °C, the formation of new clusters is assessed by light microscopy (100 × magnification). Cell culture supernatants are collected for HIV-1 p24 and HIV-2/SIVmac251 p27 core antigen measurement by ELISA. In CEMx174-infected cell cultures, which show a propensity to form syncytia induced by the virus envelope glycoproteins, syncytia are counted, in blinded fashion, by light microscopy for each well at 5 days following infection. (Only for Reference)

别名	雷特格韦, MK-0518
分子量	444.42
分子式	C20H21FN6O5
CAS No.	518048-05-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 82 mg/mL (184.5 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2501 mL	11.2506 mL	22.5012 mL	56.2531 mL
	5 mM	0.45 mL	2.2501 mL	4.5002 mL	11.2506 mL
	10 mM	0.225 mL	1.1251 mL	2.2501 mL	5.6253 mL
	20 mM	0.1125 mL	0.5625 mL	1.1251 mL	2.8127 mL
	50 mM	0.045 mL	0.225 mL	0.45 mL	1.1251 mL
	100 mM	0.0225 mL	0.1125 mL	0.225 mL	0.5625 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Hare S, et al. Proc Natl Acad Sci U S A. 2010, 107(46), 20057-220062. 2. Hicks C, et al. Clin Infect Dis. 2009, 48(7), 931-939. 3. Moss DM, et al. Antimicrob Agents Chemother. 2012, 56(6), 3020-3026. 4. Hare S, et al. Mol Pharmacol. 2011, 80(4), 565-572. 5. Lewis MG, et al. Retrovirology. 2010, 7, 21. 6. Tan S, Li W, Li Z, et al. A Novel CXCR4 Targeting Protein SDF-1/54 as an HIV-1 Entry Inhibitor. Viruses. 2019, 11(9): 874. 7. Capoci I R G, Faria D R, Sakita K M, et al. Repurposing approach identifies new treatment options for invasive fungal disease[J]. Bioorganic chemistry. 2019 Mar;84:87-97. 8. Tan S, Li J Q, Cheng H, et al. The anti-parasitic drug suramin potently inhibits formation of seminal amyloid fibrils and their interaction with HIV-1[J]. Journal of Biological Chemistry. 2019: jbc. RA118. 006797.

文献引用

1. Tan S, Li J Q, Cheng H, et al. The anti-parasitic drug suramin potently inhibits formation of seminal amyloid fibrils and their interaction with HIV-1. Journal of Biological Chemistry. 2019: jbc. RA118. 006797 2. Capoci I R G, Faria D R, Sakita K M, et al. Repurposing approach identifies new treatment options for invasive fungal disease. Bioorganic Chemistry. 2019 Mar;84:87-97 3. Tan S, Li W, Li Z, et al. A Novel CXCR4 Targeting Protein SDF-1/54 as an HIV-1 Entry Inhibitor. Viruses. 2019, 11(9): 874

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Raltegravir 518048-05-0 Microbiology/Virology Proteases/Proteasome HIV Protease Integrase 雷特格韦 HIV inhibit HIV Integrase MK0518 Inhibitor MK-0518 MK 0518 Human immunodeficiency virus inhibitor

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Raltegravir

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords