Rabeprazole-d₄ potassium  (Synonyms: 雷贝拉唑钾-d₄; LY307640-d₄ potassium)

Rabeprazole-d₄ potassium is deuterated labeled Rabeprazole sodium (HY-B0656A). Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H⁺/K⁺-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC₅₀ of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux^[1][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]。
Rabeprazole 在用 0.2 mM 处理 16 小时后减弱人胃癌细胞的细胞活力^[3]。
Rabeprazole 完全抑制 MKN-28 细胞中 ERK1/2 的磷酸化。胃癌细胞系 MKN-28 在酸性培养基 (pH 5.4) 中培养 2 小时，用 Rabeprazole (0.2 mM，持续 2 小时) 预处理可强烈抑制 MKN-28 细胞中的 ERK 1/2 磷酸化^[3]。

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

Rabeprazole sodium (10 mg/kg；口服每 48 小时一次，持续 18 周) 疗程导致雌性小鼠骨密度 (BMD) 显著下降并降低血清钙水平并产生继发性甲状旁腺功能亢进症^[4]。

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

401.56

C₁₈H₁₆D₄KN₃O₃S

雷贝拉唑钾-d₄

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]. Aly A M Shaalan, et al. Supplement With Calcium or Alendronate Suppresses Osteopenia Due to Long Term Rabeprazole Treatment in Female Mice: Influence on Bone TRAP and Osteopontin Levels. Front Pharmacol. 2020 May 13;11:583.  [Content Brief]

  [3]. Tara A Shea, et al. Identification of Proton-Pump Inhibitor Drugs That Inhibit Trichomonas Vaginalis Uridine Nucleoside Ribohydrolase. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1080-4.  [Content Brief]

  [4]. Mengli Gu, et al. Rabeprazole Exhibits Antiproliferative Effects on Human Gastric Cancer Cell Lines. Oncol Lett. 2014 Oct;8(4):1739-1744.  [Content Brief]