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Raltegravir (CAS 518048-05-0)

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Alternate Names:
MK-0518; Isentress
Application:
Raltegravir is Raltegravir is a potent integrase strand transfer inhibitor for (PFV) IN
CAS Number:
518048-05-0
Purity:
≥99%
Molecular Weight:
444.42
Molecular Formula:
C20H21FN6O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Raltegravir, also referred to as MK-0518, is an antiretroviral compound. As a human immunodeficiency virus (HIV) integrase strand transfer inhibitor (HIV-1 INSTI), raltegravir displays potent antiviral activity against HIV-1. By binding to and inhibiting the action of integrase, an essential HIV enzyme responsible for incorporating viral genetic material into the host cell′s genetic material, raltegravir effectively blocks HIV replication. This potent HIV-1 integrase inhibitor exhibits significant efficacy in inhibiting HIV-1 both in vitro and against HIV-2 in CEMx174 cells. While it does weakly inhibit hepatic cytochrome P450 activity, raltegravir is primarily recognized for its ability to effectively attenuate viral replication and combat the spread of HIV. Furthermore, raltegravir showcases its potency by sensitizing S217Q PFV IN to the same extent as the WT enzyme. In the context of acutely infected human lymphoid CD4+ T-cell lines MT-4 and CEMx174, raltegravir efficiently inhibits the replication of SIVmac251, a simian immunodeficiency virus strain.


Raltegravir (CAS 518048-05-0) References

  1. Raltegravir: the first in a new class of integrase inhibitors for the treatment of HIV.  |  Sayana, S. and Khanlou, H. 2008. Expert Rev Anti Infect Ther. 6: 419-26. PMID: 18662108
  2. New therapeutic strategies for raltegravir.  |  Garrido, C., et al. 2010. J Antimicrob Chemother. 65: 218-23. PMID: 20016017
  3. Clinical pharmacology profile of raltegravir, an HIV-1 integrase strand transfer inhibitor.  |  Brainard, DM., et al. 2011. J Clin Pharmacol. 51: 1376-402. PMID: 21209233
  4. Raltegravir-induced DRESS syndrome.  |  Loulergue, P. and Mir, O. 2012. Scand J Infect Dis. 44: 802-3. PMID: 22803794
  5. Does Once-Daily Raltegravir Have Any Role in the Antiretroviral Treatment?  |  Gutierrez-Valencia, A., et al. 2015. Medicine (Baltimore). 94: e1743. PMID: 26512567
  6. Reduced raltegravir clearance in HIV-infected liver transplant recipients: an unexpected interaction with immunosuppressive therapy?  |  Cattaneo, D., et al. 2016. J Antimicrob Chemother. 71: 1341-5. PMID: 26755497
  7. A safety evaluation of raltegravir for the treatment of HIV.  |  de Miguel, R., et al. 2018. Expert Opin Drug Saf. 17: 217-223. PMID: 29199485
  8. Maternal-Neonatal Raltegravir Population Pharmacokinetics Modeling: Implications for Initial Neonatal Dosing.  |  Lommerse, J., et al. 2019. CPT Pharmacometrics Syst Pharmacol. 8: 643-653. PMID: 31215170
  9. Raltegravir 1200 mg once daily as maintenance therapy in virologically suppressed HIV-1 infected adults: QDISS open-label trial.  |  Hall, N., et al. 2022. AIDS Res Ther. 19: 4. PMID: 35033092
  10. Raltegravir Inclusion Decreases CD4 T-Cells Intra-Cellular Viral Load and Increases CD4 and CD28 Positive T-Cells in Selected HIV Patients.  |  Kumar, G., et al. 2022. Cells. 11: PMID: 35053324
  11. Spectrum of Activity of Raltegravir and Dolutegravir Against Novel Treatment-Associated Mutations in HIV-2 Integrase: A Phenotypic Analysis Using an Expanded Panel of Site-Directed Mutants.  |  Smith, RA., et al. 2022. J Infect Dis. 226: 497-509. PMID: 35134180
  12. Optimising neonatal antiretroviral therapy using raltegravir: a qualitative analysis of healthcare workers' and caregivers' perspectives.  |  Katirayi, L., et al. 2022. BMJ Paediatr Open. 6: PMID: 36053612
  13. Pharmacokinetic interaction between raltegravir and rifampicin in an infant with HIV exposed to active TB: a case report.  |  van der Veer, MA., et al. 2022. Antivir Ther. 27: 13596535221119932. PMID: 36062614

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Raltegravir, 5 mg

sc-364600
5 mg
$100.00

Raltegravir, 50 mg

sc-364600A
50 mg
$821.00

Raltegravir, 100 mg

sc-364600B
100 mg
$1229.00

Raltegravir, 500 mg

sc-364600C
500 mg
$2861.00

Raltegravir, 1 g

sc-364600D
1 g
$4085.00