Ulipristal acetate
Based on 4 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.89%
- No. CAS: 126784-99-4
- Fòrmula: C30H37NO4
- Peso molecular:475.62
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ulipristal acetate
More
Actividad biológica
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>100 nM
Compound: 2, CBD-2914
|
Agonist activity at human PRB expressed in CHO cells
Agonist activity at human PRB expressed in CHO cells
|
[PMID: 18243712] |
| CHO | IC50 |
0.2 nM
Compound: 2, CBD-2914
|
Antagonist activity at human PRB expressed in CHO cells assessed as inhibition of Org 2058 induced-transactivation
Antagonist activity at human PRB expressed in CHO cells assessed as inhibition of Org 2058 induced-transactivation
|
[PMID: 18243712] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 126784-99-4
-
Appearance Solid
-
Peso molecular 475.62
-
Fòrmula C30H37NO4
-
Color White to off-white
-
SMILES
O=C1CCC2=C3[C@@H](C4=CC=C(N(C)C)C=C4)C[C@@]5(C)[C@](CC[C@]5(OC(C)=O)C(C)=O)([H])[C@]3([H])CCC2=C1
-
Synonyms
CDB-2914
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Coronavirus envelope protein activates TMED10-mediated unconventional secretion of inflammatory factors. [Abstract]2024 Oct 8;15(1):8708. PMID: 39379362 -
Brain Behav Immun
Chronic psychological stress-orchestrated glial-ILC3 circuit exacerbates intestinal inflammation and depression. [Abstract]2025 Nov:130:106118. PMID: 40987409 -
Hum Reprod
Effects of ulipristal acetate on human embryo attachment and endometrial cell gene expression in an in vitro co-culture system. [Abstract]2015 Apr;30(4):800-11. PMID: 25740886 -
Int J Cancer
Progesterone receptor isoform ratio dictates antiprogestin/progestin effects on breast cancer growth and metastases: A role for NDRG1. [Abstract]2022 May 1;150(9):1481-1496. PMID: 34935137
Solvente y solubilidad
DMSO : 33.33 mg/mL (70.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
-
Ficha de datos (284 KB)
-
SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Jadav SP, et al. Ulipristal acetate, a progesterone receptor modulator for emergency contraception. J Pharmacol Pharmacother. 2012 Apr;3(2):109-11. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1025 mL | 10.5126 mL | 21.0252 mL | 52.5630 mL |
| 5 mM | 0.4205 mL | 2.1025 mL | 4.2050 mL | 10.5126 mL | |
| 10 mM | 0.2103 mL | 1.0513 mL | 2.1025 mL | 5.2563 mL | |
| 15 mM | 0.1402 mL | 0.7008 mL | 1.4017 mL | 3.5042 mL | |
| 20 mM | 0.1051 mL | 0.5256 mL | 1.0513 mL | 2.6281 mL | |
| 25 mM | 0.0841 mL | 0.4205 mL | 0.8410 mL | 2.1025 mL | |
| 30 mM | 0.0701 mL | 0.3504 mL | 0.7008 mL | 1.7521 mL | |
| 40 mM | 0.0526 mL | 0.2628 mL | 0.5256 mL | 1.3141 mL | |
| 50 mM | 0.0421 mL | 0.2103 mL | 0.4205 mL | 1.0513 mL | |
| 60 mM | 0.0350 mL | 0.1752 mL | 0.3504 mL | 0.8760 mL |
Ulipristal acetate Related Classifications
HY-16508 Related Classifications
Powered by Bioz