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/ Tenofovir alafenamide

替诺福韦艾拉酚胺 /Tenofovir alafenamide {[allProObj[0].p_purity_real_show]}

货号：A138397 同义名： 替诺福韦 / GS-7340;TAF

GS-7340 is the prodrug of tenofovir which inhibits reverse transcriptase and is used to treat HIV and hepatitis B.

Tenofovir alafenamide 化学结构 CAS号：379270-37-8
Tenofovir alafenamide 化学结构
CAS号：379270-37-8
Tenofovir alafenamide 3D分子结构
CAS号：379270-37-8
Tenofovir alafenamide 化学结构 CAS号：379270-37-8
Tenofovir alafenamide 3D分子结构 CAS号：379270-37-8
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Tenofovir alafenamide 纯度/质量文件 产品仅供科研

货号：A138397 标准纯度： {[allProObj[0].p_purity_real_show]}
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Tenofovir alafenamide 生物活性

描述 Reverse transcription and integration are the defining features of the Retroviridae; the common name "retrovirus" derives from the fact that these viruses use a virally encoded enzyme, reverse transcriptase (RT), to convert their RNA genomes into DNA[3]. GS-7340 (Tenofovir alafenamide) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor. Tenofovir alafenamide (GS-7340) hemifumarate is an amidate prodrug of Tenofovir with good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF)[4]. GS-7340 antiviral activities are similar across all cell types, ranging from 5 to 7 nM. The antiviral activity of TAF (Tenofovir alafenamide) 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[5]. GS-7340 is less nephrotoxic than its predecessor prodrug, tenofovir disoproxil fumarate (TDF). GS-7340's unique pharmacokinetic profile enables provision of lower required doses for antiviral efficacy. Lower concentrations reach renal tubules minimizing intracellular accumulation and mitochondrial damage[6].

Tenofovir alafenamide 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
MT2 cells Cytotoxicity assay Cytotoxicity against human MT2 cells, CC50=40 μM 24686012

Tenofovir alafenamide 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03377608 - Completed - Uganda ... 展开 >> MU-JHU Care Ltd Kampala, Uganda 收起 <<
NCT02957864 Renal Insufficiency,Chronic ... 展开 >> Hiv Therapeutic Agent Toxicity 收起 << Phase 4 Recruiting February 2020 Netherlands ... 展开 >> Ziekenhuis Rijnstate Recruiting Arnhem, Gelderland, Netherlands Contact: Marc Claassen, PhD          MC Slotervaart Recruiting Amsterdam, Netherlands, 1066EC Contact: Saskia Vrouenraets, MD, PhD    0205129333    saskia.vrouenraets@slz.nl    OLVG Not yet recruiting Amsterdam, Netherlands, 1091AC Contact: Guido van den Berk, MD, PhD    0205999111    g.e.l.vandenberk@olvg.nl    Erasmus MC Recruiting Rotterdam, Netherlands, 3000CA Contact: ingeborg wijting, MD    0031107040704    i.wijting@erasmusmc.nl    Contact: bart rijnders, MD PhD    0031107033510    b.rijnders@erasmusmc.nl    Maasstad ziekenhuis Recruiting Rotterdam, Netherlands, 3079DZ Contact: Anna Roukens, MD, PhD    0102911911    roukensa@maasstadziekenhuis.nl 收起 <<
NCT00924898 Acute HIV Infection ... 展开 >> HIV Infections 收起 << Phase 4 Completed - United States, North Carolina ... 展开 >> The University of North Carolina - Chapel Hill Chapel Hill, North Carolina, United States, 27599 Duke University Durham, North Carolina, United States, 27707 收起 <<

Tenofovir alafenamide 参考文献

[1]Lee WA, He GX, et al. Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue. Antimicrob Agents Chemother. 2005 May;49(5):1898-906.

[2]Chapman H, Kernan M, et al. Purification of PMPA amidate prodrugs by SMB chromatography and x-ray crystallography of the diastereomerically pure GS-7340. Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):1085-90.

[3]Wei-Shau Hu,et al. HIV-1 reverse transcription. Cold Spring Harb Perspect Med. 2012 Oct 1;2(10):a006882.

[4]Babusis D, et al. Mechanism for effective lymphoid cell and tissue loading following oral administration of nucleotide prodrug GS-7340. Mol Pharm. 2013. 10(2), 459-66.

[5]Ruane PJ, 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. 63(4),449-55.

[6]Tessa K Novick,et al. Tenofovir alafenamide nephrotoxicity in an HIV-positive patient: A case report. Medicine (Baltimore). 2017. 96(36), e8046.

Tenofovir alafenamide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.49mL

2.10mL

1.05mL

20.99mL

4.20mL

2.10mL

Tenofovir alafenamide 技术信息

CAS号379270-37-8
分子式C21H29N6O5P
分子量 476.466
别名 替诺福韦 ;GS-7340;TAF
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C
溶解度

DMSO: 30 mg/mL(62.96 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: 6.5 mg/mL(13.64 mM)，配合低频超声助溶
动物实验配方

Tags: Tenofovir alafenamide | GS-7340;TAF | 替诺福韦 | Antivirus | Reverse Transcriptase Inhibitor | HBV | HIV | Reverse Transcriptase | NRTI | AmBeed-信号通路专用抑制剂 | Tenofovir alafenamide 纯度/质量文件 | Tenofovir alafenamide 生物活性 | Tenofovir alafenamide 细胞研究 | Tenofovir alafenamide 临床数据 | Tenofovir alafenamide 参考文献 | Tenofovir alafenamide 实验方案 | Tenofovir alafenamide 技术信息

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