AdipoGen Ulipristal acetate
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Chemical. CAS 126784-99-4. Formula C30H37NO4. MW 475.62. Synthetic. Ulipristal acetate is a selective progesterone receptor modulator SPRM that binds to the human progesterone receptors PR-A and PR-B EC50s=8.5 and 7.7nM, respectively, rabbit uterine PR EC50=13.6nM, and rabbit thymic glucocorticoid receptor GR EC50=15.4nM. It is selective for human progesterone receptors over the human estrogen receptor ER EC50>10,000nM. It inhibits growth of IGROV-1 and SKOV3 human ovarian cancer cells IC50s=15.5 and 31.5µM, respectively even after resistance to combined cisplatin and paclitaxel treatment has developed. Ulipristal acetate reverses the proliferative effect of progesterone on patient-derived germline mutant BRCA1 breast tissue xenografts in ovariectomized athymic mice. Formulations containing ulipristal acetate have been used as emergency contraceptives and to treat uterine fibroids.