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Tenofovir Alafenamide Hemifumarate,1392275-56-7

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    YZ剂描述:

    产品名称:Tenofovir Alafenamide Hemifumarate

    产品别名:替诺福韦艾拉酚胺半富马酸盐

    英文别名:Tenofovir alafenamide;GS7340;GS 7340

    靶点:Reverse Transcriptase

    CAS:1392275-56-7

    纯度:>98%

    外观:Powder

    保存方法:store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

    描述:GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate.

    溶解性:

    In Vitro: 

    DMSO : 50 mg/mL (93.55 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    ConcentrationSolventMass1 mg5 mg10 mg
    1 mM1.8709 mL9.3545 mL18.7091 mL
    5 mM0.3742 mL1.8709 mL3.7418 mL
    10 mM0.1871 mL0.9355 mL1.8709 mL
    *请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存方式和期限。
    In Vivo:

    请根据您的实验动物和给YF式选择适当的溶解方案,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的工作
    液,建议您现用现配,当天使用;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分比是指该溶剂在您配制终溶液中的体积占比):

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution

    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: 2.5 mg/mL (4.68 mM); Clear solution; Need warming

    *

    体外研究:

    Tenofovir disoproxil fumarate (TDF) serves as a control for CatA-independent prodrug activation. Baseline antiviral activities (mean EC50±standard deviation) obtained in the absence of a protease inhibitors (PI) are determined from 6 independent donors for GS-7340 (EC50=5.3±1.2 nM) and TDF (EC50=2.8±1.1 nM) and are used to calculate fold change EC50s from four independent donors under conditions of PI pretreatment. GS-7340 antiviral activities are similar across all cell types, ranging from 5 to 7 nM, while the CC50 varies from 4.7 to 42 μM for MT-4 and MT-2 cells, respectively. The antiviral activity of TAF is evaluated against a panel of HIV-1 and HIV-2 isolates, including HIV-1 group M subtypes A to G, as well as group N and O isolates. Overall, for the 29 primary HIV-1 isolates tested in PBMCs, TAF EC50s range from 0.1 to 12 nM, with a mean EC50 of 3.5 nM compared to a mean EC50 of 11.8 nM for AZT, which is used as an internal control. For the HIV-2 isolates, the mean EC50s are 1.8 nM for TAF and 6.4 nM for AZT.

    体内研究:GS-7340 is an amidate prodrug of Tenofovir with good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF) .

    产品信息订购:

      产品货号   产品名称   规格 价格 大包装及货期
      abs814224   Tenofovir Alafenamide Hemifumarate   100mg  3510   立即咨询

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