生物活性 | |||
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描述 | GS-7340 Fumarate (tenofovir alafenamide: TAF) is a novel nucleotide reverse transcriptase inhibitor for the treatment of HIV-1 infection that has efficacy similar to that of TDF (tenofovir disoproxil fumarate) and improved safety compared with TDF[3]. Compared with 300 mg TDF, TAF demonstrated more potent antiviral activity, higher peripheral blood mononuclear cell intracellular tenofovir diphosphate levels, and lower plasma TFV exposures, at approximately 1/10th of the dose[4]. TAF has a much lower risk of kidney toxicity or bone density changes than TDF, and also offers long-term potential in the pre-exposure prophylaxis (PrEP) of HIV infections. TAF is specifically accumulated in lymphatic tissue, and in the liver, and hence also holds great potential for the treatment of hepatitis B virus (HBV) infections[5]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.69mL 0.34mL 0.17mL |
8.44mL 1.69mL 0.84mL |
16.88mL 3.38mL 1.69mL |
参考文献 |
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