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Raltegravir potassium

Catalog No. T2239   CAS 871038-72-1
Synonyms: MK 0518 potassium salt, Raltegravir potassium salt

Raltegravir potassium (MK 0518 potassium salt) salt(MK0518 potassium salt) is a potent integrase (IN) inhibitor, used to treat HIV infection.

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Raltegravir potassium Chemical Structure
Raltegravir potassium, CAS 871038-72-1
Pack Size Availability Price/USD Quantity
10 mg In stock $ 34.00
25 mg In stock $ 61.00
50 mg In stock $ 97.00
100 mg In stock $ 178.00
200 mg In stock $ 268.00
500 mg In stock $ 453.00
1 mL * 10 mM (in DMSO) In stock $ 30.00
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Raltegravir potassium (MK 0518 potassium salt) salt(MK0518 potassium salt) is a potent integrase (IN) inhibitor, used to treat HIV infection.
In vitro PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC50 of 900 nM. PFV IN displays 10% of WT activity and is inhibited by Raltegravir with an IC50 of 200 nM which indicates an appr twofold decrease in susceptibility to the IN strand transfer inhibitor (INSTI) compared with WT IN. S217Q PFV IN is as sensitive to Raltegravir as the WT enzyme[1]. Raltegravir is metabolized by glucuronidation, not hepatically. Raltegravir has potent in vitro activity against HIV-1, with a 95% inhibitory concentration of 31±20 nM, in human T lymphoid cell cultures. Raltegravir is also active against HIV-2 when Raltegravir is tested in CEMx174 cells, with an IC95 of 6 nM. Raltegravir metabolism occurs primarily through glucuronidation. Drugs that are strong inducers of the glucuronidation enzyme, UGT1A1, significantly reduce Raltegravir concentrations and should not be used. Raltegravir exhibits weak inhibitory effects on hepatic cytochrome P450 activity. Raltegravir does not induce CYP3A4 RNA expression or CYP3A4-dependent testosterone 6-β-hydroxylase activity[2]. Raltegravir cellular permeativity is reduced in the presence of magnesium and calcium[3]. Raltegravir and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs efficiently block viral replication[4]. SIVmac251 replication is efficiently inhibited by Raltegravir, which shows an EC90 in the low nanomolar range in acutely infected human lymphoid CD4+ T-cell lines MT-4 and CEMx174[5].
In vivo Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate exhibits an undetectable viral load following Raltegravir monotherapy[5].
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.
Synonyms MK 0518 potassium salt, Raltegravir potassium salt
Molecular Weight 482.51
Formula C20H20FN6O5·K
CAS No. 871038-72-1

Storage

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

Solubility Information

DMSO: 87 mg/mL(180.3 mM)

TargetMolReferences and Literature

1. Hare, S., et al., Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance. Proc Natl Acad Sci U S A, 2010. 107(46): p. 20057-62. 2. Hicks C, et al. Raltegravir: the first HIV type 1 integrase inhibitor. Clin Infect Dis. 2009 Apr 1;48(7):931-9. 3. Moss DM, et al. Divalent metals and pH alter raltegravir disposition in vitro. Antimicrob Agents Chemother. 2012 Jun;56(6):3020-6. 4. Hare S, et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol. 2011 Oct;80(4):565-72. 5. Lewis, M.G., et al. 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. 7: p. 21.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Bioactive Compounds Library Max Drug Repurposing Compound Library Anti-Viral Compound Library Inhibitor Library NO PAINS Compound Library Clinical Compound Library Approved Drug Library PPI Inhibitor Library Anti-Infection Compound Library

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Keywords

Raltegravir potassium 871038-72-1 Microbiology/Virology Proteases/Proteasome HIV Protease Integrase Raltegravir inhibit HIV Inhibitor MK 0518 MK 0518 potassium salt Human immunodeficiency virus Raltegravir potassium salt MK-0518 MK0518 HIV Integrase MK 0518 potassium inhibitor

 

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