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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-HIV-MK-2048
MK-2048

Chemical Structure : MK-2048

CAS No.: 869901-69-9

MK-2048 (MK 2048;MK2048)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 461.87
    分子式 C21H21ClFN5O4
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    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)-

    参考文献

    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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