Ulipristal acetate

SKU: orb1305355

Description

Ulipristal acetate is a selective progesterone receptor modulator used in research to study progesterone antagonism. It is applied in investigations of uterine fibroid pathogenesis, emergency contraception mechanisms, and endometrial biology, utilizing both in vitro receptor binding assays and in vivo animal models.

Research Area

Cell Biology, Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 126784-99-4
• MW: 475.62
• Purity: >99.99% (May vary between batches)
• Formula: C₃₀H₃₇NO₄
• SMILES: CN(C)c1ccc(cc1)[C@H]1C[C@@]2(C)[C@@H](CC[C@]2(OC(C)=O)C(C)=O)[C@@H]2CCC3=CC(=O)CCC3=C12
• Target: Autophagy,Progesterone Receptor,Estrogen/progestogen Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.21 mM);DMSO:50 mg/mL (105.13 mM)

Bioactivity

• In Vivo:
  Ulipristal and CDB-4124 exhibit notable antiprogestational effects in vivo. Ulipristal acetate has been shown to reduce the occurrence of fibroadenomas and adenocarcinomas in the mammary glands across all groups studied. At the highest administered dose in rats, ulipristal acetate exposure [AUC(0-24h)] is 67 times the human therapeutic exposure at 10 mg/day. Importantly, in mice, ulipristal acetate does not lead to an increase in tumor formation, even at exposures up to 313 times the therapeutic level. Adverse effects in mice are confined to weight changes in specific organs (liver, pituitary, thyroid/parathyroid glands, and epididymis) and minimal panlobular hepatocellular hypertrophy at a dose of 130 mg/kg/day. Additionally, ulipristal acetate at doses of 1 mg/kg and 5 mg/kg causes a dose-dependent increase in endometrial thickening, observed by pathologists more frequently than in controls. There is also a minor decrease in secretory differentiation as the dose of ulipristal acetate increases, indicated by reduced sub- and supra-nuclear vacuolation.
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• In Vitro:
  Ulipristal acetate blocks activin A modulation of fibronectin and vascular endothelial growth factor A (VEGF-A) mRNA expression in cultured myometrial and leiomyoma cells. Ulipristal acetate decreases the DNA fragmentation at the 100-ng/mL dose and continuing up to the 10,000-ng/mL dose compared to those spermatozoa in the control group.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, anti-progestational, anti-fertility, anti-glucocorticoid, CDB 2914, CDB2914, CDB-2914, contraception, inhibit, NR3C3, leiomyoma, Inhibitor, Estrogen Receptor, EstrogenReceptor, emergency, PR, progestogen Receptor, ProgesteroneReceptor, progestogenReceptor, Progesterone Receptor, Ulipristal, Ulipristal Acetate, Ulipristal acetate, uterine

Compound Identifiers

PubChem CID

130904