Raltegravir (MK-0518) |
| Catalog No.GC11956 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 518048-05-0
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
MT-4 cells |
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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. |
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Reacting condition |
0.0001 ~ 1 μM; 5 days |
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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]: | |
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Animal models |
SIVmac251-infected rhesus macaques |
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Dosage form |
100 mg; p.o.; b.i.d. |
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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. |
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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. |
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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. | |
| Cas No. | 518048-05-0 | SDF | |
| 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 | ||
| 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 | ||
| Formula | C20H21FN6O5 | M.Wt | 444.4 |
| Solubility | ≥ 19.95 mg/mL in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2502 mL | 11.2511 mL | 22.5023 mL |
| 5 mM | 450 μL | 2.2502 mL | 4.5005 mL |
| 10 mM | 225 μL | 1.1251 mL | 2.2502 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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