2712343-38-7

• 常用中文名：Raltegravir-d4
• 常用英文名：Raltegravir-d4
• CAS号：2712343-38-7
• 分子式：C₂₀H₁₇D₄FN₆O₅
• 分子量：448.44
• 相关类别： 信号通路 抗感染 HIV
• 发布时间：2022-06-25 16:59:04
• 更新时间：2026-07-16 12:09:41
• Raltegravir-d4是氘标记的Raltegravir。Raltegravir是一种有效的整合酶(IN)抑制剂,用于治疗HIV感染。

名称

• 英文名: Raltegravir-d4
• 英文别名: N-[2-[5-hydroxy-1-methyl-6-oxo-4-[(2,3,5,6-tetradeuterio-4-fluorophenyl)methylcbamoyl]pyrimidin-2-yl]propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-cboxamide

物化性质

• 分子式: C₂₀H₁₇D₄FN₆O₅
• 分子量: 448.44

生物活性

• 描述: Raltegravir-d4是氘标记的Raltegravir。Raltegravir是一种有效的整合酶(IN)抑制剂,用于治疗HIV感染。
• 相关类别:
  信号通路 >> 抗感染 >> HIV
  研究领域 >> 感染
  信号通路 >> 代谢酶/蛋白酶 >> 艾滋病毒整合酶
• 体外研究: 氢、碳和其他元素的稳定重同位素已被纳入药物分子中,主要作为药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注[1]。
• 参考文献:

  [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

  [2]. Hare, S., et al., Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance. Proc Natl Acad Sci U S A, 2010. 107(46): p. 20057-62.

  [3]. 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.

  [4]. Hicks C, et al. Raltegravir: the first HIV type 1 integrase inhibitor. Clin Infect Dis. 2009 Apr 1;48(7):931-9

  [5]. Moss DM, et al. Divalent metals and pH alter raltegravir disposition in vitro. Antimicrob Agents Chemother. 2012 Jun;56(6):3020-6

  [6]. Hare S, et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol. 2011 Oct;80(4):565-72.

  [7]. Lewis, M.G., et al. Response of a simian immunodeficiency virus (SIVmac251) to raltegravir: a basis for a new treatment for simian AIDS and an animal model for studying lentiviral persistence during antiretroviral therapy. Retrovirology, 2010. 7: p. 21.