Drospirenone
Based on 1 publication(s) in Google Scholar
Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgen receptor (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. .
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- Pureza: 99.95%
- No. CAS: 67392-87-4
- Fòrmula: C24H30O3
- Peso molecular:366.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Drospirenone
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Actividad biológica
Drospirenone (10-150 µM, 24-48 h) has the value of EC50 (105 to 119 μM (24 h exposure) and 51 to 58 μM (48 h exposure)) for the cytotoxicity in PLHC-1 cells[1].
Drospirenone (10-200 µM, 15-120 min) increases ROS production in PLHC-1 cells[2].
Drospirenone (0.01-10 µM, 24 h) decreases both PAI-1 and tPA secretion in human immortalized endometrial endothelial cells (HEEC)[2].
Drospirenone (1-100 µM, 72 h) causes DNA damage to MCF-7 cells when supplemented with mice liver S9 fraction[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PLHC-1 cell
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Concentration:10-150 µM
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Incubation Time:24 h, 48 h
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Result:Caused a 50% decline in cell viability with the effective concentration of 102-119 μM after 24 h exposure and 51-58 μM after 48 h exposure.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult female mice [3]
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Dosage:10 mg/kg, 100mg/kg
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Administration:Oral gavage (p.o.)
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Result:Caused DNA damage at dose rates of 10 and 100 mg/kg. Enhanced the genotoxicity combinated with ethinylestradiol.
Chemical Information
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No. CAS 67392-87-4
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Appearance Solid
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Peso molecular 366.49
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Fòrmula C24H30O3
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Color White to off-white
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SMILES
C[C@@]12[C@](OC3=O)(CC3)[C@@H](C4)[C@@H]4[C@@]1([H])[C@@]([C@@H]5[C@H]6C5)([H])[C@]([C@](C6=CC7=O)(CC7)C)([H])CC2
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Synonyms
Dihydrospirorenone
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 50 mg/mL (136.43 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 (6.82 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.82 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Marqueño A, et al. Drospirenone induces the accumulation of triacylglycerides in the fish hepatoma cell line, PLHC-1 [J]. Science of The Total Environment, 2019, 692: 653-659. [Content Brief]
[2]. Sabouni R, et al. Drospirenone effects on the plasminogen activator system in immortalized human endometrial endothelial cells [J]. Reproductive sciences, 2021, 28: 1974-1980. [Content Brief]
[3]. Mir A H, et al. Genotoxic effects of drospirenone and ethinylestradiol in human breast cells (in vitro) and bone marrow cells of female mice (in vivo) [J]. Drug and Chemical Toxicology, 2022, 45(4): 1493-1499. [Content Brief]
[4]. Motivala A, et al. Drospirenone for oral contraception and hormone replacement therapy: are its cardiovascular risks and benefits the same as other progestogens? [J]. Drugs, 2007, 67: 647-655. [Content Brief]
[5]. Fuhrmann, U., et al., The novel progestin drospirenone and its natural counterpart progesterone: biochemical profile and antiandrogenic potential. Contraception, 1996. 54(4): p. 243-51. [Content Brief]
[6]. Muhn, P., et al., Drospirenone: a novel progestogen with antimineralocorticoid and antiandrogenic activity. Pharmacological characterization in animal models. Contraception, 1995. 51(2): p. 99-110. [Content Brief]
[7]. Warming, L., et al., Safety and efficacy of drospirenone used in a continuous combination with 17beta-estradiol for prevention of postmenopausal osteoporosis. Climacteric, 2004. 7(1): p. 103-11. [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 | 2.7286 mL | 13.6429 mL | 27.2859 mL | 68.2147 mL |
| 5 mM | 0.5457 mL | 2.7286 mL | 5.4572 mL | 13.6429 mL | |
| 10 mM | 0.2729 mL | 1.3643 mL | 2.7286 mL | 6.8215 mL | |
| 15 mM | 0.1819 mL | 0.9095 mL | 1.8191 mL | 4.5476 mL | |
| 20 mM | 0.1364 mL | 0.6821 mL | 1.3643 mL | 3.4107 mL | |
| 25 mM | 0.1091 mL | 0.5457 mL | 1.0914 mL | 2.7286 mL | |
| 30 mM | 0.0910 mL | 0.4548 mL | 0.9095 mL | 2.2738 mL | |
| 40 mM | 0.0682 mL | 0.3411 mL | 0.6821 mL | 1.7054 mL | |
| 50 mM | 0.0546 mL | 0.2729 mL | 0.5457 mL | 1.3643 mL | |
| 60 mM | 0.0455 mL | 0.2274 mL | 0.4548 mL | 1.1369 mL | |
| 80 mM | 0.0341 mL | 0.1705 mL | 0.3411 mL | 0.8527 mL | |
| 100 mM | 0.0273 mL | 0.1364 mL | 0.2729 mL | 0.6821 mL |
Drospirenone Related Classifications
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