Trimegestone-¹³C,d₃  (Synonyms: RU 27987-¹³C,d₃)

Trimegestone-¹³C,d₃ is ¹³C and deuterated labeled Trimegestone (HY-106827). Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC₅₀ value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC₅₀=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes^[1][2].

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.

346.48

C₂₁¹³CH₂₇D₃O₃

74513-62-5

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]. Wahab M, et al. Trimegestone: expanding therapeutic choices for the treatment of the menopause. Expert Opin Investig Drugs. 2001 Sep;10(9):1737-44.  [Content Brief]

  [3]. Zhang Z, et al. In vitro characterization of trimegestone: a new potent and selective progestin. Steroids. 2000 Oct-Nov;65(10-11):637-43.  [Content Brief]