500287-72-9

• 常用中文名：利匹韦林
• 常用英文名：Rilpivirine
• CAS号：500287-72-9
• 分子式：C₂₂H₁₈N₆
• 分子量：366.418
• 相关类别： 生物化工 抑制剂 微生物学(Microbiology) Reverse Transcriptase 抑制剂
• 发布时间：2018-04-04 08:00:00
• 更新时间：2026-07-03 11:01:42
• Rilpivirine (R278474; TMC278) 是 HIV 的非核苷逆转录酶抑制剂。

名称

• 中文名: 利匹韦林
• 英文名: rilpivirine
• 中文别名: 盐酸利匹韦林 Rilpivirine Hydrochloride; 利匹韦林相关杂质; 利匹韦林/利吡韦林; 利匹韦林(REVERSE TRANSCRIPTASE抑制剂); 利匹韦林,10 MM DMSO 溶液; 利吡韦林; (E)-4-((4-((4-(2-氰基乙烯基)-2,6-二甲基苯基)氨基)嘧啶-2-基)氨基)苄腈; (E)-4-((4-((4-(2-氰基乙烯基)-2,6-二甲基苯基)氨基)嘧啶-2-基)氨基)苯甲腈; (E)-4-(4-(4-(2-氰基乙烯基)-2,6-二甲基苯基氨基)嘧啶-2-基氨基)苯腈; 赖皮韦林杂质; 氘6-利匹韦林HCl; 利匹韦林-[13C6]/精确称量; 利匹韦林及中间体
• 英文别名: [3H]-Rilpivirine; Pivelin; 4-[[4-[[4-[(1E)-2-Cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile Rilpivirine R; TMC-278; Seebio Rilpivirine; Rilpivirine(R; Rilpivirine, >=; 4-[[4-[[4-[(E)-2-cyanoethenyl]-2,6-dimethyl-phenyl]amino]pyrimidin-2-yl]amino]benzonitrile //BP; 4-{[4-({4-[(1E)-2-cyanoeth-1-en-1-yl]-2,6-diMethylphenyl}amino)pyriMidin-2-yl]amino}benzonitrile; R 278474; TMC 278; R-278474; R278474; TMC278; TMC-278; (E)-4-(4-(4-(2-cyanovinyl)-2,6-diMethylphenylaMino)pyriMidin-2-ylaMino)benzonitrile; pivirine; BENZONITRILE。RILPIVIRINE; Edurant; 4-[4-[4-[(E)-2-Cyanovinyl]-2,6-dimethylphenylamino]pyrimidin; D6-Rilpivirine HCl; BENZONITRILE,4-((4-((4-((1E)-2-CYANOETHEN YL)-2,6-DIMETHYLPHENYL)AMINO)-2-PYRIMIDINYL)AMINO)-); 4-[[4-[[4-[(E)-2-Cyanovinyl]-2,6-diMethylphenyl]amino]pyriMidin-2-yl]amino]benzonitrile; 4-[[4-[[4-[(1E)-2-Cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile; Glycerol Impurity 39; Rilpivirine/TMC-278; Rilpivirine, 10 mM in DMSO; Rilpivirine(RPV); Lipavirin/Lipavirin; DB08864; 4-[[4-[4-[(E)-2-cyanoethenyl]-2,6-dimethylanilino]pyrimidin-2-yl]amino]benzonitrile; R 278474; Benzonitrile,4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-diMethylphenyl]amino]-2-pyriMidinyl]amino]; 4-{[4-({4-[(E)-2-Cyanovinyl]-2,6-dimethylphenyl}amino)-2-pyrimidinyl]amino}benzonitrile; Rilpivirin; 4-[[4-[[4-[(E)-2-cyanoethenyl]-2,6-dimethyl-phenyl]amino]pyrimidin-2-yl]amino]benzonitrile; UNII-FI96A8X663; RilpivirineQ: What is Rilpivirine Q: What is the CAS Number of Rilpivirine Q: What is the storage condition of Rilpivirine Q: What e the applications of Rilpivirine

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 634.1±65.0 °C at 760 mmHg
• 熔点: 245ºC
• 分子式: C₂₂H₁₈N₆
• 分子量: 366.418
• 闪点: 337.3±34.3 °C
• 精确质量: 366.159302
• PSA: 97.42000
• LogP: 3.63
• 外观性状: 米色粉末
• 蒸汽压: 0.0±1.9 mmHg at 25°C
• 折射率: 1.665
• 储存条件: Refrigerator

生物活性

• 描述: Rilpivirine (R278474; TMC278) 是 HIV 的非核苷逆转录酶抑制剂。
• 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:

  NNRTIs

• 体外研究: Rilpivirine(TMC278)是下一代非核苷类逆转录酶抑制剂(NNRTI),对野生型和NNRTI抗性HIV-1具有活性。 NNRTI通过结合并阻断HIV逆转录酶(一种HIV酶)起作用。这可以防止HIV复制并降低血液中的HIV含量。
• 参考文献:

  [1]. Singh K, Marchand B, Rai DK, Sharma B, Michailidis E, Ryan EM, Matzek KB, Leslie MD, Hagedorn AN, Li Z, Norden PR, Hachiya A, Parniak MA, Xu HT, Wainberg MA, Sarafianos SG.Biochemical Mechanism of HIV-1 Resistance to Rilpivirine.J Biol Chem. 2012 Sep 6.

  [2]. Schafer JJ, Short WR.Rilpivirine, a novel non-nucleoside reverse transcriptase inhibitor for the management of HIV-1 infection: a systematic review.Antivir Ther. 2012 Jul 25.

  [3]. Vingerhoets J, Rimsky L, Van Eygen V, Nijs S, Vanveggel S, Boven K, Picchio G.Preexisting mutations in the rilpivirine Phase III trials ECHO and THRIVE: prevalence and impact on virologic response.Antivir Ther. 2012 Sep 6.

  [4]. Gomes T, Juurlink DN, Mamdani MM.Comparative adherence to oxybutynin or tolterodine among older patients.Eur J Clin Pharmacol. 2012 Jan;68(1):97-9. Epub 2011 Jun 28.

  [5]. Azijn, Hilde et al. TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.Antimicrobial Agents and Chemotherapy (2010), 54(2), 718-727.

安全

• 危害码 (欧洲): Xi
• 海关编码: 2933599090

合成路线

上下游产品

上游产品  9
873-74-5 244768-32-9 24596-19-8 3095-47-4
823786-21-6 708254-90-4 87-62-7 4102-53-8
1228671-28-0
下游产品  1
700361-47-3

海关

海关编码	2933599090
中文概述	2933599090. 其他结构上有嘧啶环的化合物(包括其他结构上有哌嗪环的化合物. 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	2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%