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Cat. No. Name Size Price Add Cart
KI1323Raltegravir potassium salt5 mg$160
Raltegravir potassium salt10 mg$270
Raltegravir potassium salt50 mg$850

Chemical Characteristic

Product NameRaltegravir potassium salt
SynonymsMK-0518
CAS No.518048-05-0
Molecular Weight 444.4
FormulaC20H21FN6O5
Smiles[K] c1(nc(c(c(=O)n1C)O)C(=O)NCc1ccc(cc1)F)C(C)(NC(=O)c1oc(nn1)C)C
Chemical Structure

Biological activities

Raltegravir is a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. The IC50 of raltegravir is 15 nM against recombinant HIV-1 integrase. Raltegravir shows the antiviral activity with IC95 of 18.7 and 31 nM in 10% FBS and 50% NHS, respectively.[1] Raltegravir is metabolized by glucuronidation, not hepatically.[2] Raltegravir concentration-dependently inhibits DNA strand stransfer with an IC50 of 10 nM. Raltegravir inhibits DNA polymerase and RNase H activities of HIV-1 reverse transcriptase and human DNA polymerases ?, β and γ with IC50 of >100, >25, >50, >50 and >50 µM, respectively. The IC95 values of raltegravir in mitogen-activated human peripheral blood mononuclear cells infected with primary isolates of HIV-1 including isolates resistant to NNRTI and PI, are 6-50 nM in 20% FBS-containing clutur medium. The IC95 of raltegravir in CEMx174 human lymphoid cells infected with an HIV-2 laboratory isolate is 6.3 nM in 10% FBS-containing culture medium. In a single oral dose toxicity study in mice, raltegravir 1000, 1500, and 2000 mg/kg are administered to male and female mice. Consequently, 1 out of 3 males in the 2000 mg/kg group dies. [3]

Protocols

In vivo: Raltegravir is suspended or dissolved in 0.5% methylcellulose or polyethylene glycol/water (80:20).

References

[1] Summa V, et al. Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. J Med Chem. 2008, 51(18): 5843-5855.
[2] Raltegravir et al.Raltegravir: the first HIV type 1 integrase inhibitor. Clin Infect Dis. 2009, 48(7): 931-939.
[3] www.pmda.go.jp/english/service/pdf/Isentress.pdf

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