Zafirlukast-d₆  (Synonyms: 扎鲁司特-d₆; ICI 204219-d₆)

Zafirlukast-d₆ is deuterated labeled Zafirlukast (HY-17492). Zafirlukast (ICI 204219) is a potent orally active leukotriene D₄ (LTD₄) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.

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]。

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

Zafirlukast 是一种肽基白三烯拮抗剂和 LTD₄ 抑制剂。暴露 13 周后，两种剂量水平的 Zafirlukast (270 和 540 mg/kg)、高剂量 Zafirlukast (1200 mg/kg) 和含有 600 mg/kg 齐留通的组合显著降低了肺肿瘤的产量与 Zafirlukast 或 MK-866。含有 Zileuton 和 Zafirlukast 的组合预防肺部肿瘤的功效与单独使用任一抑制剂的功效没有显著差异。虽然当以联合用药的剂量水平单独给药时，Zileuton 或 MK-886 都不能预防肺部肿瘤；包含它们的组合确实可以显著预防肿瘤。相比之下，包含 Zafirlukast 和 MK-886 的组合不会降低肿瘤的产量，而单独使用 Zafirlukast 会显著降低肿瘤的产量^[3]。

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

581.71

C₃₁H₂₇D₆N₃O₆S

1109278-84-3

扎鲁司特-d₆

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]. Lei C, et al. Zafirlukast attenuates advanced glycation end-products (AGEs)-induced degradation of articular extracellular matrix (ECM). Int Immunopharmacol. 2019;68:68-73.  [Content Brief]

  [3]. Finnerty JP, et al. Role of leukotrienes in exercise-induced asthma. Inhibitory effect of ICI 204219, a potent leukotriene D₄ receptor antagonist. Am Rev Respir Dis. 1992 Apr;145(4 Pt 1):746-9.  [Content Brief]

  [4]. Gunning WT, et al. Chemoprevention by lipoxygenase and leukotriene pathway inhibitors of vinyl carbamate-induced lung tumors in mice. Cancer Res. 2002 Aug 1;62(15):4199-201.  [Content Brief]