Tenofovir alafenamide hemifumarate|1392275-56-7|(半富马酸替诺福韦艾拉酚胺; GS-7340 hemifumarate)-陌孚医药/Medlife

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Tenofovir alafenamide hemifumarate (Synonyms: 半富马酸替诺福韦艾拉酚胺; GS-7340 hemifumarate)

目录号: PL04388 纯度: ≥99%

CAS No. :1392275-56-7

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中文名称	Tenofovir alafenamide hemifumarate
中文别名	替诺福韦艾拉酚胺半富马酸盐;GS7340半富马酸盐;2,3-二氢-5-氨基-6-氯异吲哚酮;GS-7340半富马酸;替诺福韦艾拉芬胺半富马酸盐;替诺福韦艾拉酚胺富马酸盐;替诺福韦艾拉酚胺富马酸;替诺福韦艾拉酚胺富马酸半盐;替诺福韦艾拉芬胺半富马酸;(S)-丙胺酸异丙酯2-{(S)-[((R)-1-(6-氨基-9H-嘌呤-9-基)-1-甲基乙氧基]甲基}-苯氧基磷酰基半反丁烯二酸盐;替诺福韦-富马酸阿芬烯胺[ USAN ];替诺福韦艾拉芬胺;富马酸磷丙替诺福韦
英文名称	Tenofovir alafenamide hemifumarate
英文别名	GS7340（Tenofovir Alafenamide Fumarate）;GS-7340 Hemifumarate;Tenofovir alafenamide fumarate, 2:1;L-Alanine,N-((S)-(((1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy)methyl)phenoxyphosphinyl)-,1-methylethyl ester,(2E)-2-butenedioate (2:1);GS-7340-03;1-Methylethyl N-((S)-(((1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy)methyl)phenoxyphosphinoyl)-L-alaninate,(2E)-2-butenedioate;(E)-but-2-enedioic acid,propan-2-yl (2S)-2-[[1-(6-aminopurin-9-yl)propan-2-yloxymethyl-phenoxyphosphoryl]amino]propanoate;(S)-Isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate fumarate(2:1);Tenofovir Alafenamide Fumarate;Tenofovir alafenamide fumarate(2:1);GS7340 hemifumarate;Tenofovir alafenamide hemifumarate;N-[(S)-[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-L-alanine 1-methylethyl ester (2E)-2-butenedioate (2:1);GS 7340-03;GS-7340 (hemifumarate);L-Alanine,N-[(S)-[[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-, 1-methylethyl ester, (2E)-2-butenedioate (2:1);TENOFOVIR ALAFENAMIDE HEMIFUMARATE (GS-7340 HEMIFUMARATE);Tenofovir levamide amine fumarate;GS7340(Tenofovir Alafenamide Fumarate);(Tenofovir alafenamide : fumarate = 2:1);Anti-HIV
Cas No.	1392275-56-7
分子式	₂[C₂₁H₂₉N₆O₅P]^.C₄H₄O₄
分子量	1069.00
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) 是 Tenofovir 的前体，Tenofovir 是一种 HIV-1 核苷酸逆转录酶抑制剂。

生物活性

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.

性状

Solid

IC50 & Target[1][2]

HIV-1 HIV-2

体外研究(In Vitro)

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) 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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an amidate prodrug of Tenofovir with good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF) . has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Birkus G, et al. Intracellular Activation of Tenofovir Alafenamide and the Effect of Viral and Host Protease Inhibitors. Antimicrob Agents Chemother. 2015 Oct 26;60(1):316-22.
[2]. Callebaut C, et al. In Vitro Virology Profile of Tenofovir Alafenamide, a Novel Oral Prodrug of Tenofovir with Improved Antiviral Activity Compared to That of Tenofovir Disoproxil Fumarate. Antimicrob Agents Chemother. 2015 Oct;59(10):5909-16.

溶解度数据	In Vitro: DMSO : 50 mg/mL (93.55 mM; Need ultrasonic)H₂O : 20 mg/mL (37.42 mM; ultrasonic and warming and heat to 60°C)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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