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Drospirenone

Name: Drospirenone
Brand: TargetMol
SKU: T1541
Price: 43 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1541Cas No. 67392-87-4

Alias ZK 3059, Dihydrospirorenone

Drospirenone (ZK 3059) is a synthetic spironolactone analogue and progestin with progestational and anti-mineralocorticoid activity.

Drospirenone

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Purity: 99.97%

Catalog No. T1541Alias ZK 3059, DihydrospirorenoneCas No. 67392-87-4

Drospirenone (ZK 3059) is a synthetic spironolactone analogue and progestin with progestational and anti-mineralocorticoid activity.

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$43	In Stock	In Stock
25 mg	$78	In Stock	In Stock
50 mg	$133	In Stock	In Stock
100 mg	$217	In Stock	In Stock
200 mg	$323	In Stock	In Stock
500 mg	$543	-	In Stock
1 mL x 10 mM (in DMSO)	$48	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.97%

Color:White

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COA HNMR LCMS

Product Introduction

Drospirenone AI Summary

Drospirenone exhibits a diverse range of bioactivities and pharmacokinetic properties. It shows high oral bioavailability of 76.0% in humans and has notable activities inhibiting human tyrosyl-DNA phosphodiesterase 1 (TDP1), with potencies of 7499.3 nM without CPT and 8414.4 nM with CPT. The compound also blocks Ebola virus entry with AC50 values ranging from 3.162 µM to 39.81 µM across various assays. Additionally, it demonstrates a high affinity for the progesterone receptor (IC50 of 43.3 nM) and a lower affinity for the androgen receptor (IC50 of 630.0 nM). Pharmacokinetically, when co-administered with drospirenone and ethinyl estradiol in healthy females, Drospirenone contributes to specific bioactivity profiles including area under the curve (AUC), peak plasma concentration (Cmax), time to peak concentration (Tmax), and half-life (T1/2). Further, it inhibits bile salt export pump (BSEP) and multidrug resistance-associated protein 4 (MRP4) with IC50 values of 16400.0 nM and 37900.0 nM, respectively, and shows a steady-state concentration ratio to IC50 values of 0.006 and 0.002 respectively at a 3 mg/day dose. Regarding antiviral activity, Drospirenone has shown effects against SARS-CoV-2, demonstrating inhibition of virus-induced cytotoxicity in both Caco-2 and VERO-6 cells. Additionally, it exhibits partial inhibition of the SARS-CoV-2 3CL-Pro protease (22.97% and 8.618% inhibition at 20 µM). The compound also interacts with a wide range of receptors, including serotonin, adrenergic, dopamine, and opioid receptors, showing variable binding affinities and some agonist or antagonist activities. These findings suggest a multifaceted pharmacological profile, making Drospirenone a molecule of interest for multiple therapeutic areas..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Drospirenone (ZK 3059) is a synthetic spironolactone analogue and progestin with progestational and anti-mineralocorticoid activity.
Synonyms	ZK 3059, Dihydrospirorenone

Chemical Properties

Molecular Weight	366.49
Formula	C₂₄H₃₀O₃
Cas No.	67392-87-4
Smiles	[H][C@@]12[C@@H]3C[C@@H]3[C@@]3(CCC(=O)O3)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])[C@H]2C[C@H]2C2=CC(=O)CC[C@]12C
Relative Density.	1.26 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 9 mg/mL (24.56 mM), Sonication is recommended.

DMSO: 25.79 mg/mL (70.37 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.46 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7286 mL	13.6429 mL	27.2859 mL	136.4294 mL
5 mM	0.5457 mL	2.7286 mL	5.4572 mL	27.2859 mL
10 mM	0.2729 mL	1.3643 mL	2.7286 mL	13.6429 mL
20 mM	0.1364 mL	0.6821 mL	1.3643 mL	6.8215 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0546 mL	0.2729 mL	0.5457 mL	2.7286 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc