A selective progesterone receptor modulator (SPRM) that binds to human PR-A

Ulipristal Acetate – 50 mg

Brand:
Cayman
CAS:
126784-99-4
Storage:
-20
UN-No:
Non-Hazardous - /

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).{40657} 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 (Item No. 13119) and paclitaxel (Item No. 10461) treatment has developed.{40658} Ulipristal acetate reverses the proliferative effect of progesterone on patient-derived germline mutant BRCA1 breast tissue xenografts in ovariectomized athymic mice.{40659} Ulipristal acetate (40 mg/kg, i.p.) administered to female mice within 6 hours of human chorionic gonadotropin (hCG) treatment inhibits ovulation.{40660} Formulations containing ulipristal acetate have been used as emergency contraceptives and to treat uterine fibroids.  

 

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SKU: 23657 - 50 mg Category:

Description

A selective progesterone receptor modulator (SPRM) that binds to human PR-A, PR-B, rabbit uterine PR, and rabbit thymic GR (EC50s = 8.5, 7.7, 13.6, and 15.4 nM, respectively); 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 and paclitaxel treatment has developed; reverses the proliferative effect of progesterone on patient-derived germ-line mutant BRCA1 breast tissue xenografts in ovariectomized athymic mice; inhibits ovulation in female mice when administered within 6 h of treatment with hCG (40 mg/kg, i.p.)

Formal name: 17-(acetyloxy)-11β-[4-(dimethylamino)phenyl]-19-norpregna-4,9-diene-3,20-dione

Synonyms:  CDB 2914|HRP 2000|RU 44675

Molecular weight: 475.6

CAS: 126784-99-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology||Research Area|Cancer|Multidrug Resistance||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Endocrinology & Metabolism|Reproductive Biology

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