Ulipristal Acetate

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 7.7 nM, respectively), rabbit uterine PR (EC50 = 13.6 nM), and rabbit thymic glucocorticoid receptor (GR, EC50 = 15.4 nM). It is selective for human progesterone receptors over the human estrogen receptor (ER, EC50 = >10,000 nM). It inhibits growth of IGROV-1 and SKOV3 human ovarian cancer cells (IC50s = 15.5 and 31.5 µM, respectively) even after resistance to combined cisplatin (Cay-13119) and paclitaxel (Cay-10461) treatment has developed. Ulipristal acetate reverses the proliferative effect of progesterone on patient-derived germline mutant BRCA1 breast tissue xenografts in ovariectomized athymic mice. Ulipristal acetate (40 mg/kg, i.p.) administered to female mice within 6 hours of human chorionic gonadotropin (hCG) treatment inhibits ovulation. Formulations containing ulipristal acetate have been used as emergency contraceptives and to treat uterine fibroids.Formal Name: 17-(acetyloxy)-11beta-[4-(dimethylamino)phenyl]-19-norpregna-4,9-diene-3,20-dione. CAS Number: 126784-99-4. Synonyms: CDB 2914, HRP 2000, RU 44675. Molecular Formula: C30H37NO4. Formula Weight: 475.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.2 mg/ml. lambdamax: 265, 304 nm. SMILES: CN(C)C(C=C1)=CC=C1[C@H]2C[C@@]3(C)[C@](CC[C@]3(OC(C)=O)C(C)=O)([H])[C@]4([H])CCC5=CC(CCC5=C42)=O. InChi Code: InChI=1S/C30H37NO4/c1-18(32)30(35-19(2)33)15-14-27-25-12-8-21-16-23(34)11-13-24(21)28(25)26(17-29(27,30)3)20-6-9-22(10-7-20)31(4)5/h6-7,9-10,16,25-27H,8,11-15,17H2,1-5H3/t25-,26+,27-,29-,30-/m0/s1. InChi Key: OOLLAFOLCSJHRE-ZHAKMVSLSA-N.