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Raltegravir (MK-0518) Sale

(Synonyms: 雷特格韦; MK-0518) 目录号 : GC11956

Raltegravir (MK-0518) 是一种有效的整合酶 (IN) 抑制剂,用于治疗 HIV 感染。

Raltegravir (MK-0518) Chemical Structure

Cas No.:518048-05-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,155.00
现货
5mg
¥599.00
现货
10mg
¥1,040.00
现货
50mg
¥3,329.00
现货
100mg
¥5,460.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment [1]:

Cell lines

MT-4 cells

Preparation method

The solubility of this compound in DMSO is > 20 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.0001 ~ 1 μM; 5 days

Applications

Raltegravir inhibited SIVmac251 replication at the low nanomolar, the EC50 value of which was approximately one order of magnitude lower than that of HIV-1 IIIB. However, HIV-1 exhibited faster cytopathogenicity kinetics than SIVmac251. The results of antigen-capture ELISA assays demonstrated that in human T-cell lines, Raltegravir exhibited similar inhibition on SIVmac251 and HIV-1 replication.

Animal experiment [1]:

Animal models

SIVmac251-infected rhesus macaques

Dosage form

100 mg; p.o.; b.i.d.

Applications

In SIVmac251-infected rhesus macaques, Raltegravir significantly decreased the viral load, but only in seven days of treatment. One non-human primate showed an undetectable viral load after Raltegravir monotherapy. However, this primate had a low viral load before treatment was initiated. In addition, The combination of two NRTIs/NtRTIs plus Raltegravir stably suppressed SIVmac251 viral load, but not the proviral DNA, in non-human primates.

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]. 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.

产品描述

Raltegravir, formerly named MK-0518, is an HIV-1 integrase strand transfer inhibitor which has been shown to have activity against multidrug-resistant HIV-1 and both CCR5-trophic and CXCR4-trophic HIV-1 in vitro. Structural modifications on these molecules are made in order to maximize potency as HIV-integrase inhibitors against the wild type virus, a selection of mutants, and optimize the selectivity, pharmacokinetic, and metabolic profiles in preclinical species. Raltegravir derives from the evolution of 5,6-dihydroxypyrimidine-4-carboxamides and N-methyl-4-hydroxypyrimidinone-carboxamides. It has been shown to have potent antiretroviral effects, with a mean decrease from baseline in HIV-1 RNA concentrations of about 2 log10 copies per mL after 10 days of monotherapy.

Reference

[1].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.
[2].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.

Chemical Properties

Cas No. 518048-05-0 SDF
别名 雷特格韦; MK-0518
化学名 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
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
分子式 C20H21FN6O5 分子量 444.4
溶解度 ≥ 19.95 mg/mL in DMSO 储存条件 4°C, protect from light
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2502 mL 11.2511 mL 22.5023 mL
5 mM 0.45 mL 2.2502 mL 4.5005 mL
10 mM 0.225 mL 1.1251 mL 2.2502 mL
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