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Tenofovir alafenamide fumarate

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Chemical Structure| 379270-38-9 同义名 : GS-7340 fumarate;TAF fumarate
CAS号 : 379270-38-9
货号 : A167277
分子式 : C25H33N6O9P
纯度 : 98%
分子量 : 592.538
MDL号 : MFCD28167823
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 35 mg/mL(59.07 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 25 mg/mL(42.19 mM)

动物实验配方:
生物活性
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
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

[1]Ruane PJ, DeJesus E, et al. Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults. J Acquir Immune Defic Syndr. 2013 Aug 1;63(4):449-55.

[2]Koziol E, Skalicka-Wozniak K. Imperatorin-pharmacological meaning and analytical clues: profound investigation. Phytochem Rev. 2016;15:627-649.

[3]Gibson AK, Shah BM, Nambiar PH, Schafer JJ. Tenofovir Alafenamide. Ann Pharmacother. 2016 Nov;50(11):942-952

[4]Ruane PJ, DeJesus E, Berger D, Markowitz M, Bredeek UF, Callebaut C, Zhong L, Ramanathan S, Rhee MS, Fordyce MW, Yale K. Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults. J Acquir Immune Defic Syndr. 2013 Aug 1;63(4):449-55

[5]De Clercq E. Tenofovir alafenamide (TAF) as the successor of tenofovir disoproxil fumarate (TDF). Biochem Pharmacol. 2016 Nov 1;119:1-7