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Ulipristal acetate (also known as CDB-2914) is a potent and selective SPRM (selective progesterone receptor modulator) for emergency contraception after an unprotected intercourse or contraceptive failure. Ulipristal acetate has partial agonistic as well as antagonistic effects on the progesterone receptor. It also binds to the glucocorticoid receptor, but has no relevant affinity to the estrogen, androgen and mineralocorticoid receptors. Ulipristal acetate dose dependently suppressed progesterone-induced acrosome reaction and hyperactivation in human spermatozoa.
| ln Vitro |
In leiomyoma cells, ulipristal acetate (0.1–5 μM; 96 h) promotes autophagy. Ulipristal produced alterations in the expression of the autophagy markers p62/SQSTM1 and LC3. In leiomyoma cells, ulipristal upregulates the Atg7 protein [2]. In cultured uterine fibroids and leiomyoma cells, ulipristalacetate inhibits the regulation of activin A on fibronectin and vascular endothelial growth factor A (VEGF-A) mRNA expression [4].
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| ln Vivo |
In vivo, ulipristal and CDB-4124 exhibit strong anti-pregnancy properties [5]. In all therapy groups, ulipristal acetate decreased the incidence of adenocarcinoma and breast fibroadenoma. Rats exposed to the highest dose of ulipristal acetate [AUC (0-24h)] were exposed to 67 times the therapeutic dose of 10 mg/day in humans. When ulipristal acetate was administered in doses up to 313 times the therapeutic exposure, mice showed no growth in tumors of any kind. The liver, pituitary, thyroid/parathyroid, and epididymis weight alterations, as well as the smallest entire lobule in male and female mice given a dose of 130 mg/kg/day, were the only findings linked to ulipristal acetate in mice. enlargement of hepatocytes [6]. When compared to the control, ulipristal acetate (1 mg/kg and 5 mg/kg) increased in a dose-dependent way the frequency of pathologist assessment of endometrial thickening. Both secretory differentiation and the frequency of subnuclear and supranuclear vacuole formation somewhat decrease with an increase in ulipristal acetate dosage [7].
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| References |
[1]. Jadav SP, et al. Ulipristal acetate, a progesterone receptor modulator for emergency contraception. J Pharmacol Pharmacother. 2012 Apr;3(2):109-11.
[2]. Del Bello B, et al. Autophagy up-regulation by ulipristal acetate as a novel target mechanism in the treatment of uterine leiomyoma: an in vitro study. Fertil Steril. 2019 Dec;112(6):1150-1159. [3]. Hild SA, et al. CDB-2914: anti-progestational/anti-glucocorticoid profile and post-coital anti-fertility activity in rats and rabbits. Hum Reprod. 2000 Apr;15(4):822-9. [4]. Ciarmela P, et al. Ulipristal acetate modulates the expression and functions of activin a in leiomyoma cells. Reprod Sci. 2014 Sep;21(9):1120-5. [5]. Attardi BJ, et al. In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol. [6]. Pohl O, et al. Carcinogenicity and chronic rodent toxicity of the selective progesterone receptor modulator ulipristal acetate. Curr Drug Saf. 2013 Apr;8(2):77-97. [7]. Pohl O, et al. A 39-week oral toxicity study of ulipristal acetate in cynomolgus monkeys. Regul Toxicol Pharmacol. 2013 Jun;66(1):6-12 |
| Molecular Formula |
C30H37NO4
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| Molecular Weight |
475.6191
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| CAS # |
126784-99-4
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| Related CAS # |
Ulipristal;159811-51-5;Ulipristal acetate-d6;1621894-64-1
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| SMILES |
O(C(C([H])([H])[H])=O)[C@]1(C(C([H])([H])[H])=O)C([H])([H])C([H])([H])[C@@]2([H])[C@]3([H])C([H])([H])C([H])([H])C4=C([H])C(C([H])([H])C([H])([H])C4=C3[C@@]([H])(C3C([H])=C([H])C(=C([H])C=3[H])N(C([H])([H])[H])C([H])([H])[H])C([H])([H])[C@@]21C([H])([H])[H])=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~70.08 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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