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Raltegravir (MK-0518) is a novel HIV-1 integrase strand transfer inhibitor with potent in vitro activity against wild-type and multi-class resistant HIV-1 virus (in vitro IC95 for HIV-1 in 50% normal human serum = 33 nM). Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. Raltegravir is administered orally every 12h and does not require boosting with low-dose ritonavir (RTV) to achieve therapeutic concentrations.
| Molecular Weight | 482.51 |
| Formula | C20H20FKN6O5 |
| CAS Number | 871038-72-1 |
| Solubility (25°C) | DMSO 10 mg/mL Water 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Rosa de Miguel, et al. A safety evaluation of raltegravir for the treatment of HIV
[3] Emma D Deeks. Raltegravir Once-Daily Tablet: A Review in HIV-1 Infection
| Related Integrase Products |
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| BMS-707035
BMS-707035 is an HIV-1 integrase (IN) inhibitor. HIV-1 integrase (IN) represents a therapeutically advantageous viral target to treat HIV/AIDS in the clinic. |
| Elvitegravir
Elvitegravir (EVG) is a HIV integrase inhibitor with IC50 of 0.7 nM, 2.8 nM and 1.4 nM for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD, respectively. |
| Raltegravir
Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively. |
| MK-2048
MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively. |
| Dolutegravir
Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. |
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