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Purity: ≥98%
Drospirenone (MSp; SH-470; ZK-30595; LF-111; Slynd; Yasminelle; Yaz; Nextstellis) is a synthetic progestogen approved for used as an oral contraceptive alone or in combination with other medicaitons (Trade name: Alone: Slynd; With estradiol: Angeliq; With ethinylestradiol: Yasmin, Yasminelle, Yaz, others With estetrol: Nextstellis). It has anti-mineralocorticoid and antiandrogenic properties. Numerous oral contraceptives contain this medication. Following drospirone's binding to the progesterone receptor, a complex is formed that binds to particular sites on DNA and becomes activated. This causes changes in the endometrium and cervical mucus in addition to suppressing LH activity and inhibiting ovulation. This makes it harder for sperm to enter the uterus and implant.
| Targets |
progestogen Receptor
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|---|---|
| ln Vitro |
The toxic effects of drospirenone (10-150 μM, 24-48 h) on PLHC-1 cells had effective concentration limits (EC50 values) of 105-119 μM for 24 hours and 51-58 μM for 48 hours [1]. Drospirenone (0.01-10 µM, 24 h) inhibits PAI-1 and tPA in HEEC aqueous solutions [2]. Cellular ROS generation in PLHC-1 at -200 µM for 15-120 min [2]. Addition of 100 µM, 72 h) to the mouse model S9 component can damage DNA in MCF-7 cells [3].
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| ln Vivo |
In both male and female mice, oral dospirenone (10–100 mg/kg) for five days damages the DNA in the bone marrow cells [3].
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| Cell Assay |
Cytotoxicity assay [1]
Cell Types: PLHC-1 Cell Tested Concentrations: 10-150 µM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: Cell viability diminished by 50%, effective concentration after 24 hrs (hours) was 102-119μM, effective after 48 hrs (hours) The concentration is 51-58μM. |
| Animal Protocol |
Animal/Disease Models: Adult female mice [3]
Doses: 10 mg/kg, 100mg/kg Route of Administration: po (oral gavage) Experimental Results: DNA damage was induced at dose rates of 10 and 100 mg/kg. Concomitant use with ethinyl estradiol enhances genotoxicity. |
| References |
[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.
[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. [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. [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. [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. [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. [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. |
| Molecular Formula |
C24H30O3
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|---|---|
| Molecular Weight |
366.49
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| Exact Mass |
366.21949
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| Elemental Analysis |
C, 78.65; H, 8.25; O, 13.10
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| CAS # |
67392-87-4
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| Related CAS # |
Drospirenone-d4;2376035-94-6;Drospirenone-d4-1
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| Appearance |
Solid powder
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| SMILES |
C[C@]12CCC(=O)C=C1[C@@H]3C[C@@H]3[C@@H]4[C@@H]2CC[C@]5([C@H]4[C@@H]6C[C@@H]6[C@@]57CCC(=O)O7)C
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| InChi Key |
METQSPRSQINEEU-HXCATZOESA-N
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| InChi Code |
InChI=1S/C24H30O3/c1-22-6-3-12(25)9-17(22)13-10-14(13)20-16(22)4-7-23(2)21(20)15-11-18(15)24(23)8-5-19(26)27-24/h9,13-16,18,20-21H,3-8,10-11H2,1-2H3/t13-,14+,15-,16+,18+,20-,21+,22-,23+,24+/m1/s1
|
| Chemical Name |
(1R,2R,4R,10R,11S,14S,15S,16S,18S,19S)-10,14-dimethylspiro[hexacyclo[9.8.0.02,4.05,10.014,19.016,18]nonadec-5-ene-15,5'-oxolane]-2',7-dione
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| Synonyms |
Drospirenona; Drospirenone; Dehydrospirorenone; dihydrospirorenone; drospirenone; Drospirenonum; ZK 3059; ZK30595
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| HS Tariff Code |
2934.99.9001
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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: 50~73 mg/mL (136.4~199.2 mM)
Ethanol: ~12 mg/mL (~32.7 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.82 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 (6.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7286 mL | 13.6429 mL | 27.2859 mL | |
| 5 mM | 0.5457 mL | 2.7286 mL | 5.4572 mL | |
| 10 mM | 0.2729 mL | 1.3643 mL | 2.7286 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06039826 | Recruiting | Drug: Drospirenone Drug: Ethinyl Estradiol |
Overweight | Eli Lilly and Company | September 12, 2023 | Phase 1 |
| NCT04792385 | Active Recruiting |
Drug: E4/DRSP 15/3 mg combined tablet |
Safety | Estetra | December 28, 2020 | Phase 3 |
| NCT05675644 | Not yet recruiting | Drug: Drospirenone-only pill | Contraception | University of Colorado, Denver | February 2023 | Phase 2 |
| NCT05461573 | Recruiting | Drug: Drospirenone | Contraception Change in Bone Mineral Density |
Insud Pharma | August 2, 2022 | Phase 3 |
| NCT05156879 | Recruiting | Drug: Drospirenone ethinyl estradiol Drug: Aspirin |
Pelvic Pain | Women's Hospital School Of Medicine Zhejiang University |
December 23, 2021 | Phase 4 |
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