Trimegestone-13C,d3

Product Specifications

UNSPSC 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].

Target Antigen

Androgen Receptor; Isotope-Labeled Compounds; Phosphatase; Progesterone Receptor

Type

Isotope-Labeled Compounds

Related Pathways

Metabolic Enzyme/Protease;Others;Vitamin D Related/Nuclear Receptor

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Endocrinology

Solubility

10 mM in DMSO

Smiles

C[C@@]12[C@](CC[C@]2(C)C([C@@H](O)[13C]([2H])([2H])[2H])=O)([H])[C@@]3([H])C(CC1)=C4C(CC3)=CC(CC4)=O

Molecular Weight

346.48

References & Citations

[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.