Product Description: 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].
Applications: Metabolism-sugar/lipid metabolism
Formula: C21 13CH27D3O3
References: [1]Wahab M, et al. Trimegestone: expanding therapeutic choices for the treatment of the menopause. Expert Opin Investig Drugs. 2001 Sep;10(9):1737-44. /[2]Zhang Z, et al. In vitro characterization of trimegestone: a new potent and selective progestin. Steroids. 2000 Oct-Nov;65(10-11):637-43. /[3]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
Molecular Weight: 346.48
Research Area: Endocrinology
Solubility: 10 mM in DMSO
Target: Androgen Receptor;Isotope-Labeled Compounds;Phosphatase;Progesterone Receptor