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Raltegravir

Catalog No. T2239L   CAS 518048-05-0
Synonyms: MK-0518

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Raltegravir Chemical Structure
Raltegravir, CAS 518048-05-0
Pack Size Availability Price/USD Quantity
2 mg In stock $ 38.00
5 mg In stock $ 58.00
10 mg In stock $ 106.00
25 mg In stock $ 192.00
50 mg In stock $ 318.00
100 mg In stock $ 473.00
1 mL * 10 mM (in DMSO) In stock $ 58.00
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Purity: 100%
Purity: 99.05%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 Integrase (WT PFV):90 nM, Integrase (S217Q PFV):40 nM
Kinase Assay 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.
Cell Research 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)
Synonyms MK-0518
Molecular Weight 444.42
Formula C20H21FN6O5
CAS No. 518048-05-0

Storage

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

Solubility Information

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

DMSO: 82 mg/mL (184.5 mM)

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

TargetMolReferences and Literature

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.

TargetMolCitations

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

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library NO PAINS Compound Library FDA-Approved & Pharmacopeia Drug Library PPI Inhibitor Library Anti-Infection Compound Library Fluorochemical Library Drug Repurposing Compound Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library Clinical Compound Library

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Keywords

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

 

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