2. Vitamin D Related/Nuclear Receptor
  3. Progesterone Receptor Androgen Receptor
  4. Drospirenone

Drospirenone  (Synonyms: Dihydrospirorenone)

Cat. No.: HY-B0111 Purity: 98.45%
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Solubility

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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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Drospirenone Chemical Structure

Drospirenone Chemical Structure

CAS No. : 67392-87-4

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Based on 1 publication(s) in Google Scholar

Other Forms of Drospirenone:

Drospirenone Related Antibodies

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Description

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. [1][2][3][4].

In Vitro

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.

Drospirenone Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: PLHC-1 cell
Concentration: 10-150 µM
Incubation Time: 24 h, 48 h
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.
In Vivo

Drospirenone (10-100 mg/kg, oral gavage for five days) caused DNA damage in bone marrow cells of adult female mice[3].

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

Animal Model: Adult female mice [3]
Dosage: 10 mg/kg, 100mg/kg
Administration: Oral gavage (p.o.)
Result: Caused DNA damage at dose rates of 10 and 100 mg/kg.
Enhanced the genotoxicity combinated with ethinylestradiol.
Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT00302848Center for Epidemiology and Health Research, Germany|Bayer Healthcare Pharmaceuticals, Inc.+Bayer Schering Pharma
Contraception
November 2000
NCT01511822AGUNCO Obstetrics and Gynecology Centre
PCOS|Polycystic Ovary Syndrome
Phase 4
NCT01519401Catholic University of the Sacred Heart
Polycystic Ovary Syndrome|Estro-progestin Drugs
February 2010Not Applicable
Molecular Weight

366.49

Formula

C24H30O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References

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
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Drospirenone Related Classifications

Keywords:

Drospirenone67392-87-4DihydrospirorenoneProgesterone ReceptorAndrogen ReceptorNR3C3PLHC-1 cellshuman immortalized endometrial endothelial cellsMCF-7 cellProgestinInhibitorinhibitorinhibit

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