1392275-56-7

• 常用中文名：替诺福韦艾拉酚胺富马酸盐
• 常用英文名：Tenofovir Alafenamide Hemifumarate
• CAS号：1392275-56-7
• 分子式：C₄₆H₆₂N₁₂O₁₄P₂
• 分子量：1069.0
• 相关类别： 原料药 人工合成抗感染类药 抗病毒类药
• 发布时间：2018-09-25 18:31:14
• 更新时间：2026-06-30 12:06:37
• 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。

名称

• 中文名: 替诺福韦艾拉酚胺半富马酸盐
• 英文名: Tenofovir Alafenamide Hemifumarate
• 中文别名: 富马酸磷丙替诺福韦(替诺福艾拉盼胺); 泰诺福韦艾拉酚胺富马酸(2:1); 富马酸丙酚替诺福韦, 替诺福韦艾拉酚胺富马酸盐, Tenofovir alafenamide fumate (TAF); 替诺福韦-阿拉芬酰胺半富马酸盐[USAN; 诺福韦艾拉酚胺半富马酸盐; 替诺福韦艾拉酚胺富马酸盐(TAF); 丙酚替诺福韦原料药; 替诺福韦艾拉酚胺中间体1392-7; 富马酸泰诺福韦艾拉酚胺; 富马酸磷丙替诺福韦(替诺福韦艾拉酚胺); 富马酸丙酚替诺福韦(TAF); 替诺福韦艾拉酚氨半富马酸; 泰诺福韦艾拉酚胺半富马酸盐; 泰诺福韦二吡呋酯富马酸; 替诺福韦艾拉酚胺半富马酸; 富马酸丙酚替诺福韦; 富马酸磷丙替诺福韦; 半富马酸盐GS7340; 替诺福韦艾拉芬胺; GS-7340半富马酸盐; 富马酸丙酚替诺福韦 (富马酸替诺福韦艾拉酚胺); 富马酸丙分替诺福韦; 替诺福韦艾拉酚胺版富马酸盐; 替诺福韦-阿拉芬胺半富马酸盐[USAN]; 富马酸丙芬替诺福韦; (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; 替诺福韦艾拉酚胺富马酸盐(2:1); 富马酸丙酚替诺佛韦; GS-7340 (HEMIFUMATE)|||TENOFOVIR ALAFENAMIDE FUMATE|||替诺福韦艾拉酚胺富马酸盐; 替诺福韦-富马酸阿芬烯胺[ USAN ]; 富马酸替诺福韦艾拉芬胺; 替诺福韦艾拉芬胺半富马酸; 替诺福韦艾拉酚胺富马酸半盐; 泰诺福韦艾拉酚胺富马酸(2:1) CRS; 替诺福韦艾拉芬胺半富马酸盐; (((((R)-1-(6-氨基-9H-嘌呤-9-基)丙烷-2-基)氧基)甲基)(苯氧基)磷酰基)-L-丙氨酸异丙基 半富马酸盐; 替诺福韦艾拉酚胺富马酸; L-丙氨酸,N-[(S)-[[(1R)-2-(6-氨基-9H-嘌呤-9基)-1-甲基乙氧基]甲基]苯氧基氧膦基],1-甲基乙基酯,(2E)丁烯二酸(2:1); 泰诺福韦艾拉酚胺富马酸; 替诺福韦ALAFENAMIDE富马酸酯; N-[(S)-[[(1R)-2-(6-氨基-9H-嘌呤-9-基)-1-甲基乙氧基]甲基]苯氧基氧膦基]-L-丙氨酸异丙酯半富马酸盐
• 英文别名: Anti-HIV; Isopropyl N-[(S)-({[(2R)-1-(6-amino-9H-purin-9-yl)-2-propanyl]oxy}methyl)(phenoxy)phosphoryl]-L-alaninate (2E)-2-butenedioate (2:1); GS-7340 Hemifumarate; TAF(Tenofovir Alafenamide Hemifumate); 3H-1,2,4-Triazole-3-thione,4-amino-2,4-dihydro-5-(10-methoxyphenyl); Tenofovir Alafenamide Hemifumate salt; Tenofovir Alafenamide Hemifumate(2:1); TENOFOVIR ALAFENAMIDE HEMIFUMATE (GS-7340 HEMIFUMATE); Tenofovir alafenamide hemifumate (GS-7340); L-Alanine, N-[(S)-[(1S)-[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-, 1-methylethyl ester, (2E)-2-butenedioate (2:1); enofovir Alafenamide Fumarate; (R)-isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate fumate; Tenofovir Alafenamide Fumate //BP; (Tenofovir alafenamide : fumate = 2:1); GS-7340 (hemifumate); 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); Tenofovir Alafenamide fumate; (E)-but-2-enedioic acid,propan-2-yl (2S)-2-[[1-(6-aminopurin-9-yl)propan-2-yloxymethyl-phenoxyphosphoryl]amino]propanoate; Tenofovir Alafenamide Fumate API; 1-Methylethyl N-((S)-(((1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy)methyl)phenoxyphosphinoyl)-L-alaninate; Tenofovir Alafenamid; Tenofovir Alafenamide fumate [USAN]; Tenofovir Alafenamide fumateQ: What is Tenofovir Alafenamide fumate Q: What is the CAS Number of Tenofovir Alafenamide fumate; GS-7340-03; Tenofovir alafenamide hemifumate; GS7340(Tenofovir Alafenamide Fumate); 1-Methylethyl N-((S)-(((1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy)methyl)phenoxyphosphinoyl)-L-alaninate,(2E)-2-butenedioate; Tenofovir Alafenamide Hemifumate(2:1) CRS; (S)-isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate hemifumate; Tenofovir levamide amine fumate; Tenofovir alafenamide fumarate; Celiprolol Impurity 8(Celiprolol Impurity H); (S)-Isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate fumate(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); Isopropyl (((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alaninate hemifumate; 2-fluoro-5-[(4' -0x'H-phthalazin-1'-yl)methyllbenzoic acide'; API-Anti-HBV; Tenofovir alafenamide hemifumate, 10 mM in DMSO; Phosphonoformic Acid Fumate; N-[(S)-[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-L-alanine 1-methylethyl ester (2E)-2-butenedioate (2:1); Tenofovir dipivoxil phenol amine fumate; N-[(S)-[[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-, 1-methylethyl ester; GS-7340 (hemifumarate); Tenofovir Alafenamide Hemifumate salt[USAN; GS-7340 (hemifumate)|||Tenofovir alafenamide fumate; Alafenamide hemifumate

物化性质

• 分子式: C₄₆H₆₂N₁₂O₁₄P₂
• 分子量: 1069.0
• 精确质量: 1068.39836869
• PSA: 381.18000
• LogP: 7.60180
• 储存条件: 2-8°C

生物活性

• 描述: 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。
• 相关类别:
  信号通路 >> 抗感染 >> HIV
  信号通路 >> 抗感染 >> 逆转录酶
  研究领域 >> 感染
• 靶点:

  HIV-1, NRTIs[1]

• 体外研究: 所有细胞类型的替诺福韦艾拉酚胺(GS-7340)抗病毒活性相似,范围为5至7 nM,而MT-4和MT-2细胞的CC50分别为4.7至42μM。针对一组HIV-1和HIV-2分离株评估TAF的抗病毒活性,包括HIV-1组M亚型A至G,以及N和O组分离株。总体而言,对于在PBMC中测试的29种初级HIV-1分离株,TAF EC50的范围为0.1至12nM,平均EC50为3.5nM,而AZT的平均EC50为11.8nM,其用作内部对照。对于HIV-2分离株,TAF的平均EC50为1.8 nM,AZT的平均EC50为6.4 nM [2]。
• 体内研究: 替诺福韦艾拉酚胺(GS-7340)是替诺福韦的酰胺类前药,与替诺福韦地索普西富马酸盐(TDF)相比具有良好的口服生物利用度并增加血浆稳定性[1]。
• 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.

安全

• 危害码 (欧洲): Xi