379270-38-9|替诺福韦阿拉芬酰胺富马酸酯|Tenofovir alafenamide fumarate|-范德生物科技公司

替诺福韦阿拉芬酰胺富马酸酯

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names：
Tenofovir alafenamide fumarate
CAS号：
379270-38-9
MDL Number：
MF(分子式)： C25H33N6O9P MW(分子量)： 592.54
EINECS: Reaxys Number:
Pubchem ID:68516365 Brand:BIOFOUNT

替诺福韦阿拉芬酰胺富马酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]也称为替诺福韦阿拉芬酰胺半富马酸盐；TAF GS-7340是核苷酸逆转录酶抑制剂和替诺福韦的新型前药。吉利德科学公司正在开发它，用于治疗HIV感染。与常用的逆转录酶抑制剂富马酸替诺福韦二甲氧吡啶（Viread）密切相关，与该药剂相比，替诺福韦阿拉芬酰胺具有更大的抗病毒活性和更好的向淋巴组织的分布。吉利德（Gilead）宣布了一项三阶段临床试验，该试验评估了将GS-7340与考比司他，恩曲他滨和elvitegravir组合使用的单片方案，并计划与cobicistat，恩曲他滨和蛋白酶抑制剂darunavir共同配制该药物。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
YZM000631-10mg	10mg	99.78%	¥ 911.00	¥ 911.00		2-3天	- +	¥ 0.00
YZM000631-5mg	5mg	99.78%	¥ 585.00	¥ 585.00		2-3天	- +	¥ 0.00

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中文别名	替诺福韦阿拉芬酰胺富马酸酯(379270-38-9);替诺福韦艾拉酚胺富马酸盐;替诺福韦阿拉芬酰胺富马酸盐;替诺福韦阿拉芬酰胺半富马酸盐; GS-7340富马酸酯; GS 7340富马酸酯; GS7340富马酸酯; （S）-异丙基2-（（（（S）-（（（（R）-1-（6-amino-9H-purin-9-yl）prop-2--2-yl）oxy）甲基）（苯氧基）磷酰基）氨基）丙酸酯富马酸酯; TAF；GS734; GS-734；GS 7340；替诺福韦阿拉芬酰胺富马酸酯; 商品名称：Genvoya;
英文别名	Tenofovir alafenamide fumarate(379270-38-9);GS-7340 (fumarate); GS-7340 fumarate; GS 7340 fumarate; GS7340 fumarate; (S)-isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate fumarate; TAF; GS734; GS-734; GS 7340; Tenofovir alafenamide fumarate; trade name;
CAS号	379270-38-9
SMILES	NC1=NC=NC2=C1N=CN2C[C@@H](C)OC[P@](OC3=CC=CC=C3)(N[C@@H](C)C(OC(C)C)=O)=O.O=C(O)/C=C/C(O)=O
Inchi	InChI=1S/C21H29N6O5P.C4H4O4/c1-14(2)31-21(28)16(4)26-33(29,32-17-8-6-5-7-9-17)13-30-15(3)10-27-12-25-18-19(22)23-11-24-20(18)27;5-3(6)1-2-4(7)8/h5-9,11-12,14-16H,10,13H2,1-4H3,(H,26,29)(H2,22,23,24);1-2H,(H,5,6)(H,7,8)/b;2-1+/t15-,16+,33-;/m1./s1
InchiKey	MEJAFWXKUKMUIR-BVSQZBJNSA-N
分子式 Formula	C25H33N6O9P
分子量 Molecular Weight	592.54
闪点 FP
熔点 Melting point	No data available
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility	生物体外In Vitro:DMSO溶解度≥ 36 mg/mL(60.76 mM)H2O≥ 25 mg/mL(42.19 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性状	白色至类白色固体粉末,Power
储藏条件 Storage conditions	-20°C 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

替诺福韦阿拉芬酰胺富马酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:GS-7340 (fumarate)试剂,GS-7340 (fumarate)杂质,GS-7340 (fumarate)中间体,GS-7340 (fumarate)合成,GS-7340 (fumarate)密度,GS-7340 (fumarate)溶解度,GS-7340 (fumarate)旋光度,GS-7340 (fumarate)闪点,GS-7340 (fumarate)购买,

产品说明	替诺福韦阿拉芬酰胺富马酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]是 Tenofovir 的前体,Tenofovir是一种有效的HIV-1核苷酸逆转录酶的抑制剂
Introduction	替诺福韦阿拉芬酰胺富马酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]is an investigational oral prodrug of Tenof ovir. Tenof ovir is aHIVnucleotide reverse transcriptase inhibitor.
Application1	Tenofovir alafenamide fumarate (GS-7340 fumarate) 是 Tenofovir 的前体，Tenofovir 是一种 HIV-1 核苷酸逆转录酶抑制剂。
Application2
Application3

替诺福韦阿拉芬酰胺富马酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]药理学：

1、替诺福韦阿拉芬酰胺富马酸酯，也称为替诺福韦阿拉芬酰胺半富马酸盐；TAF GS-7340是核苷酸逆转录酶抑制剂和替诺福韦的新型前药。吉利德科学公司正在开发它，用于治疗HIV感染。与常用的逆转录酶抑制剂富马酸替诺福韦二甲氧吡啶（Viread）密切相关，与该药剂相比，替诺福韦阿拉芬酰胺具有更大的抗病毒活性和更好的向淋巴组织的分布。吉利德（Gilead）宣布了一项三阶段临床试验，该试验评估了将GS-7340与考比司他，恩曲他滨和elvitegravir组合使用的单片方案，并计划与cobicistat，恩曲他滨和蛋白酶抑制剂darunavir共同配制该药物。

2、替诺福韦阿拉法酰胺富马酸酯（GS-7340富马酸酯）是替诺福韦的前体，替诺福韦是一种HIV-1核苷酸逆转录酶抑制剂。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

替诺福韦阿拉芬酰胺富马酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]危害标识：

象形图
信号	Warning
GHS危险说明	The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.
GHS危险说明	H373 (100%): Causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure]
防范说明代码	P260, P314, and P501
防范说明代码	(The corresponding statement to each P-code can be found at the GHS Classification page.)

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

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 Aug 1;63(4

替诺福韦阿拉芬酰胺富马酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]参考文献：

1.Adenine: an important drug scaffold for the design of antiviral agents.
Wang C;Song Z;Yu H;Liu K;Ma X Acta Pharm Sin B. 2015 Sep;5(5):431-41. doi: 10.1016/j.apsb.2015.07.002. Epub 2015 Sep 2.

Adenine derivatives, in particular the scaffold bearing the acyclic nucleoside phosphonates (ANPS), possess significant antiviral and cytostatic activity. Till now, several effective adenine derivatives have been marketed for the treatment of HIV, HBV, CMV and other virus-infected diseases. These compounds are represented by tenofovir (PMPA), a medicine for both HIV and HBV, and adefovir as an anti-HBV agent. More than this, other analogs, such as GS9148, GS9131, and GS7340, are also well-known anti-viral agents that have been progressed to the clinical studies for their excellent activity. In general, the structures of these compounds include an adenine nucleobase linked to a phosphonate side chain. Considerable structural modifications on the scaffold itself and the peripheral sections were made. The structure-activity relationships (SARs) of this skeleton will provide valuable clues to identify more effective adenine derivatives as antiviral drugs. Here, we systematically summarized the SARs of the adenine derivatives, and gave important information for further optimizing this template.

2、Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults
Peter J Ruane 1, Edwin DeJesus, Daniel Berger, Martin Markowitz, U Fritz Bredeek, Christian Callebaut, Lijie Zhong, Srini Ramanathan, Martin S Rhee, Marshall W Fordyce, Kitty Yale

Abstract Objective: To evaluate the antiviral activity, safety, pharmacokinetics, and pharmacokinetics/pharmacodynamics of short-term monotherapy with tenofovir alafenamide (TAF), a next-generation tenofovir (TFV) prodrug. Design: A phase 1b, randomized, partially blinded, active- and placebo-controlled, dose-ranging study. Methods: Treatment-naive and experienced HIV-1-positive adults currently off antiretroviral therapy were randomized to receive 8, 25, or 40 mg TAF, 300 mg tenofovir disoproxil fumarate (TDF), or placebo, each once daily for 10 days. Results: Thirty-eight subjects were enrolled. Baseline characteristics were similar across dose groups. Significant reductions in plasma HIV-1 RNA from baseline to day 11 were observed for all TAF dose groups compared with placebo (P < 0.01), with a median decrease of 1.08-1.73 log10 copies per milliliter, including a dose-response relationship for viral load decrease up to 25 mg. At steady state, 8, 25, and 40 mg TAF yielded mean TFV plasma exposures [area under the plasma concentration-time curve (AUCtau)] of 97%, 86%, and 79% lower, respectively, as compared with the TFV exposures observed with 300 mg TDF. For 25 and 40 mg TAF, the mean intracellular peripheral blood mononuclear cell tenofovir diphosphate AUCtau was ∼7-fold and ∼25-fold higher, relative to 300 mg TDF. Conclusions: 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. This may translate into greater antiviral efficacy, a higher barrier to resistance, and an improved safety profile relative to TDF, supporting further investigation of TAF dosed once daily in HIV-infected patients.

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