1. APIs
  2. Nestorone
  3. Nestorone Metabolites
  4. 3α,5α-tetrahydronestorone

3α,5α-tetrahydronestorone

Structure

Notes

120 times less potent PR activity than Nestorone in human PR (hPR) transactivation assay (EC50 = 24 pM for NES vs. 2850 pM for metabolite). GC/MS-MS.

References

  1. Kumar, N.; Fagart, J.; Liere, P.; Mitchell, S. J.; Knibb, A. R.; Petit-Topin, I.; Rame, M.; El-Etr, M.; Schumacher, M.; Lambert, J. J.; Rafestin-Oblin, M. E.; Sitruk-Ware, R., Nestorone(R) as a Novel Progestin for Nonoral Contraception: Structure-Activity Relationships and Brain Metabolism Studies. Endocrinology 2017, 158 (1), 170-182.
    2. (View all citations for this reference)