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MK-2048

Chemical Structure : MK-2048

CAS No.: 869901-69-9

MK-2048 (MK 2048;MK2048)

Catalog No.: PC-43481Not For Human Use, Lab Use Only.

MK-2048 is a potent inhibitor of HIV-1 integrase (IN) and IN mutant R263K with IC50 of 2.6 nM and 1.5 nM, respectively.

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    Biological Activity

    MK-2048 is a potent inhibitor of HIV-1 integrase (IN) and IN mutant R263K with IC50 of 2.6 nM and 1.5 nM, respectively.
    MK-2048 inhibits subtype B and subtype C integrase activities with IC50 of 75 nM and 80 nM, respectively.
    MK-2048 inhibits S217H intasome with an IC50 of 900 nM, remains fully active against the N224H intasome with IC50 of 25 nM.
    MK-2048 displays substantially lower dissociation rates compared with raltegravir, another integrase inhibitor.

    Physicochemical Properties

    M.Wt 461.87
    Formula C21H21ClFN5O4
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    Pyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-4-carboxamide, 2-[(3-chloro-4-fluorophenyl)methyl]-8-ethyl-1,2,6,7,8,9-hexahydro-10-hydroxy-N,6-dimethyl-1,9-dioxo-, (6S)-

    References

    1. Quashie PK, et al. J Virol. 2012 Mar;86(5):2696-705.

    2. Van Wesenbeeck L, et al. Antimicrob Agents Chemother. 2011 Jan;55(1):321-5.

    3. Bar-Magen T, et al. J Virol. 2010 Sep;84(18):9210-6.

    4. Marsden MD, et al. Antimicrob Agents Chemother. 2011 Aug;55(8):3696-702.

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