Formulation: A solid
Formal Name: 13-ethyl-17α-hydroxy-18,19-dinorpregn-4-en-20-yn-3-one, oxime
Purity: ≥95%
Formula Markup: C21H29NO2
Formula Weight: 327,5
Shelf life (days): 1460
CAS Number: 53016-31-2
Notes: Norelgestromin is an active metabolite of the progestin norgestimate (Item No. 16547).{65297} Norelgestromin is formed from norgestimate via deacetylation in human liver microsomes. It is an agonist of the progesterone receptor and estrogen receptor α (ERα; EC50s = 11.1 and 43.4 nM, respectively) and an antagonist of the glucocorticoid and mineralocorticoid receptors (IC50s = 255 nM and 83.7 nM, respectively).{65299} Norelgestromin selectively binds to progestin receptors (IC50 = 4.61 nM for rabbit uterine receptors) over androgen receptors (IC50 = 222 nM for rat prostatic receptors) in radioligand binding assays.{53983} However, norelgestromin (1 nM) activates the androgen receptor in a transactivation assay in MDA-MB-231 breast cancer cells expressing the human receptor.{65298} Formulations containing norelgestromin in combination with ethynyl estradiol have been used as contraceptives and in the treatment of acne vulgaris in women.
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