Rupintrivir-d₇  (Synonyms: AG7088-d₇)

Rupintrivir-d7 is a deuterated labeled Rupintrivir^[1]. Rupintrivirvr (AG7088), an antiviral agent, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC₅₀ of 0.023 μM. Rupintrivirvr shows immune-modulatory effect^[2][3].

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。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
在 H1-HeLa 和 MRC-5 细胞保护试验中，Rupintrivirvr (AG7088) 抑制所有 HRV 血清型 (48 种中的 48 种) 的复制，平均 50% 有效浓度 (EC₅₀) 为 0.023 μM 和平均 EC₉₀ 为 0.082 μM 以及相关的小核糖核酸病毒，包括柯萨奇病毒 A21 和 B3、肠道病毒 70 和埃可病毒 11^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Rupintrivirvr (AG7088) 减少离体 HDM 致敏小鼠精密切割肺切片 (PCLS) 中 RV 诱导的 TH-2 细胞因子 IL-4^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

605.71

C₃₁H₃₂D₇FN₄O₇

223537-30-2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

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

  [2]. Patick AK, et al. In vitro antiviral activity of AG7088, a potent inhibitor of human rhinovirus 3C protease. Antimicrob Agents Chemother. 1999 Oct;43(10):2444-50.  [Content Brief]

  [3]. Danov O, et al. Rupintrivir reduces RV-induced TH-2 cytokine IL-4 in precision-cut lung slices (PCLS) of HDM-sensitized mice ex vivo. Respir Res. 2019 Oct 22;20(1):228.  [Content Brief]

  [4]. Dragovich PS, et al. Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 3. Structure-activity studies of ketomethylene-containing peptidomimetics. J Med Chem. 1999 Apr 8;42(7):1203-12.  [Content Brief]