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MK-0518 (Raltegravir) | HIV-1 integrase inhibitor

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Catalog #:

Product Description

Raltegravir (Isentress)is an first-in-class, orally-available, oxadiazole-based inhibitor of HIV-1 integrase, inhibiting strand transfer in vitro with an IC50 of 2-7 nM. [1] It is >1000-fold more selective for HIV-1 integrase when compared to other phosphoryltransferases, such as the polymerase and RNase H activities of HIV-1 reverse transcriptase and the human polymerases alpha, beta, and gamma.

Raltegravir has a IC95 in human T lymphoid cell cultures of 31 nM and was also active against HIV-2 when tested in CEMx174 cells, with an IC95 of 6nM. [2]

Raltegravir has been shown to be a potent and selective against Xenotropic murine leukemia-related retrovirus (XMRV) at submicromolar concentrations in MCF-7 breast cancer (EC50 = 5 nM, EC90 = 3.5 uM) and LNCaP prostate cancer (EC50 = 30 nM, EC90 0.46 um) cell lines. [3]

Technical information:

Chemical Formula:   C20H21FN6O5
CAS #:   871038-72-1
Molecular Weight:   444.42
Purity:   >98%
Appearance:   White
Chemical Name:   N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(2-(2-methyl-1,3,4-oxadiazole-5-carboxamido)propan-2-yl)-6-oxo-1,6-dihydropyrimidine-4-carboxamide
Solubility:   Up to 100 mM in DMSO
Synonyms:   Raltegravir, MK-0518, MK0518, Isentress

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


1. Temesgen et al., Raltegravir: first in class HIV integrase inhibitor. Ther. Clin. Risk Management, 2008, 4(2), 493-500. Pubmed ID: 18728839
2. Hicks et al., Raltegravir: the first HIV type 1 integrase inhibitor. Clin. Infect. Dis. 2009, 48(7), 931-939. Pubmed ID: 19231980
3. Singh et al., Raltegravir is a potent inhibitor of XMRV, a virus implicated in prostate cancer and chronic fatigue syndrome. PloS ONE 2010, 4(4), e9948. Pubmed ID: 20376347

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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