202138-50-9

• 常用中文名：富马酸替诺福韦酯
• 常用英文名：Tenofovir Disoproxil Fumarate
• CAS号：202138-50-9
• 分子式：C₂₃H₃₄N₅O₁₄P
• 分子量：635.515
• 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：2018-02-04 08:00:00
• 更新时间：2026-06-30 17:27:32
• Tenofovir Disoproxil Fumarate是用于治疗 HIV 和慢性乙型肝炎的核苷酸逆转录酶抑制剂。

名称

• 中文名: 富马酸替诺福韦酯
• 英文名: tenofovir disoproxil fumarate
• 中文别名: 替诺福韦API 富马酸替诺福韦酯; 富马酸替诺佛韦脂; 替诺福韦富马酸(标准品); 替诺福韦(富马酸盐); 替诺福韦/替诺福韦酯富马酸盐/富马酸替诺福韦酯; Tenofovir Disoproxil Fumate 富马酸替诺福韦酯，S1400; 替诺福韦杂质11; (R)-(((((1-(6-氨基-9H-嘌呤-9-基)丙烷-2-基)氧基)甲基)磷酰基)双(氧基)双(亚甲基)二异丙基二碳酸酯 富马酸盐; 泰诺福韦酯富马酸盐 标准品; 富马酸替诺福韦酯,10 MM DMSO 溶液; 替诺福韦二吡呋酯 富马酸酯; 替诺福韦富马酸替诺福韦二吡呋酯; 富马酸替诺福韦二吡; 富马酸泰诺福韦二吡呋酯; 富马酸替诺福韦二吡呋脂; 富马酸替诺福韦酯 标准品; 富马酸泰诺福韦酯; 富马酸替诺福韦二吡呋酯片补充杂质TDF; 富马酸替诺福韦二吡呋酯原料药; 富马酸泰诺福韦酯异构体; 替诺福韦/替诺福韦酯富马酸盐; 替诺福韦酯延胡索酸盐; 富马酸替诺福韦; 泰诺福韦酯费用; 富马酸替诺福韦酯202-9; 泰诺福韦酯; 替诺福韦杂质138 富马酸盐; 替诺福韦富马酸; 替诺福韦杂质115 富马酸盐; 替诺福韦地索普西富马酸盐; 抑制剂Tenofovir Disoproxil Fumate; 富马酸替诺福韦二吡呋酯; 替诺福韦二丙酸酯; (R)-9-(2-磷酸甲氧基丙基)腺嘌呤二(异丙氧羰基氧甲基)酯富马酸盐; 泰诺福韦酯富马酸盐; 富马酸替诺福韦二匹夫酯; 富马酸替诺福韦酯;泰诺福韦酯; 富马酸替诺福韦醋; 富马酸替诺福韦酯 Tenofovir Disoproxil fumate; 2,4,6,8-四氧杂-5-磷杂萘二酸,5-[[(1R)-2-(6-氨基-9H-嘌呤-9-基)-1-甲基乙氧基]甲基]-,1,9-双异丙酯,5-氧化物,富马酸盐; 富马酸替诺福韦二吡呋酯片; 替诺福韦二丙酸酯富马酸盐; Tenofovir Disoproxil Fumate 富马酸替诺福韦酯,S1400; 富马酸替诺福韦酯 CRS; 富马酸泰偌福韦酯; 泰诺福韦脂; 替诺福韦酯富马酸
• 英文别名: Tenofovir Disoproxil fumateQ: What is Tenofovir Disoproxil fumate Q: What is the CAS Number of Tenofovir Disoproxil fumate Q: What is the storage condition of Tenofovir Disoproxil fumate Q: What e the applications of Tenofovir Disoproxil fumate; GS-4331-05; 2,4,6,8-Tetraoxa-5-phosphanonanedioic acid, 5-[[(1R)-2-(6-amino-9H-purin-9-yl)-1-Methylethoxy]Methyl]-, 1,9-bis(1-Methylethyl) ester, 5-oxide, (2E)-2-butenedioate; Bis(neopentyloc)pmpa; 2,4,6,8-Tetraoxa-5-phosphanonanedioic acid, 5-[[2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]-, bis(2,2-dimethylpropyl) ester, 5-oxide, (R); (1R)-2-(6-aminopurin-9-yl)-1-methyl-ethoxy]methyl-(isopropoxycbonyloxymethoxy)phosphoryl]oxymethyl isopropyl cbonate; GS-1278 Disoproxil Fumate; Tenofovir Disoproxil Fumate; Tenofovir disoproxil D12 fumate; 202-9Tenofovir disoproxil fumate; Bis{[(isopropoxycarbonyl)oxy]methyl} ({[(2R)-1-(6-amino-9H-purin-9-yl)-2-propanyl]oxy}methyl)phosphonate (2E)-2-butenedioate (1:1); Tenofovir dipivoxil FuMate(TDF); Tenofovir diisoproxil fuMate; Tenofovir DF; 9-((R)-2-((Bis(((isopropoxycarbonyl)oxy)methoxy)phosphinyl)methoxy)propyl)adenine Fumarate; Tenofovir disoproxil Impurity 11; GS 4; Tenofovir Disproxil FuMate; 9-((R)-2-((Bis(((isopropoxycbonyl)oxy)methoxy)phosphinyl)methoxy)propyl)adenine fumate; (R)-(((((1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)bis(oxy))bis(methylene) diisopropyl bis(cbonate), fumic acid; enofovir disoproxil fuMate; Tenofovir (Disoproxil Fumarate); Tenofovir Impurity 138 Fumate; Bis(((isopropoxycarbonyl)oxy)methyl) (((1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy)methyl)phosphonate (2E)-2-Butenedioate; TENOFOVIR DISOPROXIL FUMATE [DRUG SUBSTANCE(NON-STERILE)]; FuMic acid tenofovir ester; acide (2E)-but-2-ènedioïque - {[(1R)-2-(6-amino-9H-purin-9-yl)-1-méthyléthoxy]méthyl}phosphonate de bis({[(1-méthyléthoxy)carbonyl]oxy}méthyle) (1:1); Bis{[(isopropoxycarbonyl)oxy]methyl} ({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)phosphonate (2E)-but-2-enedioate (1:1); Tenofovir disoproxil fumate 9-((R)-2-((Bis(((isopropoxycbonyl)oxy)methoxy)phosphinyl)methoxy)propyl)adenine fumate; Tenofovir disoproxil fumate RS; Tenofovir Disoroxil Fumate; Tenofovir disoproxil fumate - Bio-X; 1,3-Benzodioxole-5-cboxaldehyde,12-methoxy; Tenofovir disoproxil fumate //BP; bis{[(isopropoxycbonyl)oxy]methyl} ({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)phosphonate (2E)-but-2-enedioate (1:1); 5-[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]-2,4,6,8-tetraoxa-5-phosphanonanedioic Acid 1,9-Bis(1-methylethyl) Ester 5-Oxide (2E)-2-Butenedioate; Tenofovir Disoproxil Fumate, 10 mM in DMSO; Tenofovir disoproxil fumarate; Tenofovir Disoproxil Dumate; Viread; bis({[(1-methylethoxy)carbonyl]oxy}methyl) {[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl}phosphonate (2E)-but-2-enedioate; Tenofovir disoproxil fumate, >=; 2,4,6,8-Tetraoxa-5-phosphanonanedioic acid, 5-[[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]-, 1,9-bis(1-methylethyl) ester, 5-oxide, (2E)-2-butenedioate (1:1); Tenofovir Disoproxil Fumate (USFDA); Tenofovir Disoproxil Fumate (TDF); Tenofovir Disoproxil Fumate CRS; GS4331-05; Viread (TN); Aids-031697; Tenofovir diisoproxil fuMarate; Carbonic acid, [[[[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl][[[(1-methylethoxy)carbonyl]oxy]methoxy]phosphinyl]oxy]methyl 1-methylethyl ester, (2E)-2-butenedioate (1:1); bis({[(propan-2-yloxy)carbonyl]oxy}methyl) ({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)phosphonate (2E)-but-2-enedioate (1:1); Tenofovir Disoproxil Fumate (Tenofovir DF); GS-433105; Tenofovir dipivoxil Fumate; (R)-(((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)bis(oxy))bis(methylene) di; Disoproxil fumate; Tenofovir Disoproxil FuMate I; TENOFOVIR DISOPROXIL FUMATE (NON-STERILE DRUG SUBSTANCE); Aids031697; (((((1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)Methyl)phosphoryl)bis(oxy))bis(Methylene) diisopropyl dicbonate fuMate; Tenofovir Impurity 115 Fumate; TENOFOVIR DISOPROXIC

物化性质

• 密度: 1.45 g/cm3
• 沸点: 642.7ºC at 760 mmHg
• 熔点: 219ºC
• 分子式: C₂₃H₃₄N₅O₁₄P
• 分子量: 635.515
• 闪点: 342.5ºC
• 精确质量: 635.183960
• PSA: 269.85000
• LogP: 3.32860
• 外观性状: 白色至粉红色结晶
• 蒸汽压: 2.06E-16mmHg at 25°C
• 储存条件: Refrigerator

生物活性

• 描述: Tenofovir Disoproxil Fumarate是用于治疗 HIV 和慢性乙型肝炎的核苷酸逆转录酶抑制剂。
• 相关类别:
  信号通路 >> 抗感染 >> HBV
  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
• 体外研究: 替诺福韦在HK-2细胞中显示出对细胞活力的细胞毒性作用,在MTT测定中48和72小时的IC50值分别为9.21和2.77μM。替诺福韦降低HK-2细胞中的ATP水平。替诺福韦(3.0至28.8μM)增加HK-2细胞中的氧化应激和蛋白质羰基化。此外,替诺福韦诱导HK-2细胞凋亡,并且通过线粒体损伤诱导细胞凋亡[1]。配制在0.25％HEC中的替诺福韦和M48U1各自抑制活化的PBMC中R5-向性HIV-1BaL和X4-向性HIV-1IIIb的复制,并抑制几种实验室菌株和源自患者的HIV-1分离株。 M48U1和替诺福韦在0.25％HEC中的组合制剂显示出对抗R5-向性HIV-1BaL感染的协同抗逆转录病毒活性,并且对PBMC无毒性[2]。
• 体内研究: 施用于BLT小鼠的替诺福韦地索普西富马酸盐(20,50,140或300mg/kg)显示在BLT人源化小鼠的阴道HIV攻击期间的剂量依赖性活性。替诺福韦地索普西富马酸盐(50,140,300 mg/kg)显着降低BLT小鼠的HIV传播[3]。替诺福韦地索普西富马酸盐(0.5,1.5或5.0mg/kg /天,po)诱导长期感染WHV的土拨鼠血清病毒血症的剂量依赖性下降。替诺福韦地索普西富马酸盐给药在慢性HBV感染的土拨鼠模型中是安全有效的[4]。
• 细胞实验: 将细胞接种到48孔组织培养板（39,000个细胞/ mL）中并使其生长48小时，然后用载体或替诺福韦处理。在治疗期后，使用MTT测定评估细胞活力。 MTT测定依赖于四唑鎓染料3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四唑溴化物（MTT）通过NAD（P）H-依赖性氧化还原酶转化为甲..
• 动物实验: 将20只成年慢性WHV携带者土拨鼠按年龄，性别，体重和血清GGT活性分成5个治疗组，每组4只动物：（i）替诺福韦地索普西富马酸盐，每天15.0 mg / kg，（ii）替诺福韦Disoproxil富马酸盐5.0mg / kg /天，（iii）替诺福韦地索普西富马酸盐1.5mg / kg /天，（iv）替诺福韦地索普西富马酸盐0.5mg / kg /天，和（v）安慰剂对照。每天处理土拨鼠4周，并在停止药物治疗后再观察12周。
• 参考文献:

  [1]. Murphy RA, et al. Establishment of HK-2 Cells as a Relevant Model to Study Tenofovir-Induced Cytotoxicity. Int J Mol Sci. 2017 Mar 1;18(3)

  [2]. Musumeci G, et al. M48U1 and Tenofovir combination synergistically inhibits HIV infection in activated PBMCs and human cervicovaginal histocultures. Sci Rep. 2017 Feb 1;7:41018

  [3]. Wahl A, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model. Sci Rep. 2017 Feb 1;7:41098

  [4]. Menne S, Cote PJ, Korba BE, Antiviral effect of oral administration of tenofovir disoproxil fumarate in woodchucks with chronic woodchuck hepatitis virus infection. Antimicrob Agents Chemother. 2005 Jul;49(7):2720-8.

  [5]. Xu P, et al. Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692.

安全

• 符号: GHS05
• 信号词: Danger
• 危害声明: H318
• 警示性声明: P280-P305 + P351 + P338 + P310
• 危害码 (欧洲): Xi
• 风险声明 (欧洲): R36/37/38
• 安全声明 (欧洲): 26-36
• 危险品运输编码: NONH for all modes of transport
• 海关编码: 2933990090

合成路线

35180-01-9 110-17-8 147127-20-6 ~% 202138-50-9

文献：US2013/5969 A1, ; Page/Page column 4 ;

1215085-38-3 110-17-8 ~% 202138-50-9

文献：WO2011/111074 A2, ; Page/Page column 8; 9 ;

14047-28-0 ~% 202138-50-9

文献：Organic Process Research and Development, , vol. 14, # 5 p. 1194 - 1201

180587-75-1 ~% 202138-50-9

文献：Organic Process Research and Development, , vol. 14, # 5 p. 1194 - 1201

147127-20-6 ~% 202138-50-9

文献：Organic Process Research and Development, , vol. 14, # 5 p. 1194 - 1201

66224-66-6 ~% 202138-50-9

文献：Organic Process Research and Development, , vol. 14, # 5 p. 1194 - 1201

上下游产品

上游产品  7
35180-01-9 110-17-8 147127-20-6 1215085-38-3
14047-28-0 180587-75-1 66224-66-6
下游产品  0

海关

海关编码	2933990090
中文概述	2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素	品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%