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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 |
[1] Anton Pozniak, et al. Raltegravir in patients with tuberculosis
[3] Rosa de Miguel, et al. A safety evaluation of raltegravir for the treatment of HIV
[4] Emma D Deeks. Raltegravir Once-Daily Tablet: A Review in HIV-1 Infection
| Related Integrase Products |
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| Bictegravir Sodium
Bictegravir (GS-9883) Sodium is a novel and potent inhibitor of HIV-1 integrase, specifically targets IN strand transfer activity with an IC50 of 7.5 nM. |
| Lavendustin B
Lavendustin B inhibits HIV-1 integrase (IN) interaction with its cognate cellular cofactor lens epithelium-derived growth factor (LEDGF/p75). Lavendustin B is an inhibitor of Tyrosine Kinase and also a competitive inhibitor of glucose transporter 1 (Glut1). |
| Bictegravir
Bictegravir (GS-9883) is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM. |
| Dolutegravir sodium
Dolutegravir sodium is a potent, second generation HIV integrase inhibitor (IC₅₀ = 2.7 nM) that displays potent antiviral activity. |
| 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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