Promegestone  (Synonyms: R-5020; Surgestone)

Promegestone (R-5020), a progestin, is a potent progesterone receptor (PR) agonist. Promegestone has the potential for endocrine regulation and cancer research^[1].

Promegestone (R-5020; 1 nM) is efficient ligand with a full agonist response profile and a low EC₅₀ of 0.33 nM) in HELN-hPR while it only partially induced luciferase activity in U2OS-zfPR (EC₅₀=1.93 nM)^[1].
Promegestone is inactive in HELN cells that express luciferase but no functional receptor^[1].
Promegestone (10 nM) robustly stimulates SLC37A2 expression in cells expressing SUMO-deficient PR, but not in cells expressing WT PR in T47D cell models^[3].

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

Promegestone (R-5020; 8 mg/kg; intramuscularly)-treated pregnant mice on day 18 postbreeding has the least deterioration in extracellular collagen (lowest OD) and highest cell density compared to other groups on the day before birth^[2].

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

326.47

C₂₂H₃₀O₂

34184-77-5

Solid

White to off-white

C[C@@]12[C@](C)(CC[C@]1([C@@]3(CCC4=CC(CCC4=C3CC2)=O)[H])[H])C(CC)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Clémentine Garoche, et al. Human and Zebrafish Nuclear Progesterone Receptors Are Differently Activated by Manifold Progestins. Environ Sci Technol. 2020 Aug 4;54(15):9510-9518.  [Content Brief]

  [2]. Michael A Kirby, et al. Progesterone Receptor-Mediated Actions Regulate Remodeling of the Cervix in Preparation for Preterm Parturition. Reprod Sci. 2016 Nov;23(11):1473-1483.  [Content Brief]

  [3]. Todd P Knutson, et al. Posttranslationally modified progesterone receptors direct ligand-specific expression of breast cancer stem cell-associated gene programs. J Hematol Oncol. 2017 Apr 17;10(1):89.  [Content Brief]