Raltegravir (MK-0518) Chemical Structure
BMS-707035 is an HIV-1 integrase (IN) inhibitor.
Elvitegravir (EVG, JTK-303, GS-9137) is an inhibitor of the integrase enzyme and inhibits HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 values of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
S/GSK1349572 (GSK 1349572) is a novel potent integrase inhibitor with an IC50 of 2.7 nM in vitro.
Elvitegravir (EVG, JTK-303, GS-9137) is an inhibitor of the integrase enzyme and inhibits HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 values of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
Maraviroc is a CCR5 antagonist. Maraviroc was active (IC90) at low nanomolar concentrations against HIV-1 Ba-L.
Vicriviroc Malate is a CCR5(cellular coreceptor 5) inhibitor, in vitro activity against HIV (IC90<13 nM)
BMS-707035 is an HIV-1 integrase (IN) inhibitor.
Stavudine is a nucleoside analog reverse transcriptase inhibitor (NARTI) active against HIV.
Tenofovir (Viread) belongs to nucleotide analogue reverse transcriptase inhibitors (nRTIs).
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). Inhibition of integrase prevents insertion of HIV DNA into the human DNA genome, thus blocking the ability of HIV to replicate. Raltegravir is administered orally every 12h and does not require boosting with low-dose ritonavir (RTV) to achieve therapeutic concentrations. Raltegravir is not a potent inhibitor or inducer of cytochrome P450 3A4, and it is predominantly metabolized by glucuronidation, specifically by the enzyme UDP-glucuronosyltransferase 1A1. [1]Results from clinical trials indicate that raltegravir is safe and highly effective in the treatment of both antiretroviral-naïve and -experienced patients. [2,3]
| Molecular Weight (WM): | 444.42 |
|---|---|
| Formula: | C20H21FN6O5 |
| CAS No.: | 871038-72-1 |
| Synonyms: |
Isentress
|
| Dissolve in (25°C): | DMSO ≥89mg/mL |
| Water ≥89mg/mL | |
| Ethanol ≥2mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules
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