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Ulipristal acetate (Synonyms: CDB-2914)

Cat. No.: HY-16508 Purity: 99.93%
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Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.

For research use only. We do not sell to patients.

Ulipristal acetate Chemical Structure

Ulipristal acetate Chemical Structure

CAS No. : 126784-99-4

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Based on 1 publication(s) in Google Scholar

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Description

Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma[1][2].

In Vitro

Ulipristal acetate (0.1-5 μM; 96 hours) stimulates autophagy in leiomyoma cells. Ulipristal-induced expression changes of the autophagic markers LC3 and p62/SQSTM1. Ulipristal up-regulates Atg7 protein in leiomyoma cells[2].
Ulipristal acetate blocks activin A modulation of fibronectin and vascular endothelial growth factor A (VEGF-A) mRNA expression in cultured myometrial and leiomyoma cells[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ulipristal and CDB-4124 have significant antiprogestational activity in vivo[5].
Ulipristal acetate decreases incidences of fibroadenomas and adenocarcinomas in the mammary gland in all treated groups. Ulipristal acetate exposure [AUC(0-24h)] at the highest dose in rats is 67 times human therapeutic exposure at 10 mg/day. In mice, no tumor of any type increases at Ulipristal acetate exposures up to 313 times of therapeutic exposure. Ulipristal acetate-related findings in mice are limited to organ weight changes in the liver, pituitary, thyroid/parathyroid glands, and epididymis as well as minimal panlobular hepatocellular hypertrophy in male and female mice receiving 130 mg/kg/day[6].
Ulipristal acetate (1 mg/kg and 5 mg/kg) increases the frequency with which pathologists assessed the endometrium as being thickened compared to controls in a dose-dependent manner. There is a slight decrease in secretory differentiation with increasing dose of Ulipristal acetate, with small decreases in frequency of sub- and supra-nuclear vacuolation[7].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

475.62

Formula

C₃₀H₃₇NO₄

CAS No.

126784-99-4

SMILES

O=C1CCC2=C3[[email protected]@H](C4=CC=C(N(C)C)C=C4)C[[email protected]@]5(C)[[email protected]](CC[[email protected]]5(OC(C)=O)C(C)=O)([H])[[email protected]]3([H])CCC2=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (70.08 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1025 mL 10.5126 mL 21.0252 mL
5 mM 0.4205 mL 2.1025 mL 4.2050 mL
10 mM 0.2103 mL 1.0513 mL 2.1025 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[5]

The study consisted of four groups, each comprising four female cynomolgus monkeys. The groups eitherreceive ASV (control), or Ulipristal acetate at dose levels of 1, 5, or 25 mg/kg for 39 weeks. Two additional animals are allocated to the control and high dose groups for an 8-week post-dose recovery period. At randomization, there is no statistically significant difference between treatment groups in mean body weight. The vehicle or Ulipristal acetate is administered to all groups by oral gavage for 273 consecutive days at a dose volume of 2 mL/kg. Following the dosing or recovery period, animals are euthanized by intravenous administration of sodium pentobarbital followed by exsanguination of the femoral vessels.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

UlipristalCDB-2914CDB2914CDB 2914Progesterone ReceptorAutophagyNR3C3emergencycontraceptionuterineleiomyomaanti-progestationalanti-glucocorticoidanti-fertilityInhibitorinhibitorinhibit

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Ulipristal acetate
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HY-16508
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