1. Vitamin D Related/Nuclear Receptor Immunology/Inflammation Neuronal Signaling Membrane Transporter/Ion Channel
  2. Progesterone Receptor Androgen Receptor Glucocorticoid Receptor GABA Receptor
  3. Chlormadinone acetate

Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABAA receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders.

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Chlormadinone acetate

Chlormadinone acetate Chemical Structure

CAS No. : 302-22-7

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Based on 1 publication(s) in Google Scholar

Other Forms of Chlormadinone acetate:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABAA receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders[1][2][3].

In Vitro

Chlormadinone acetate binds to the human progesterone receptor in MCF-7 cell cytosol with a Ki value of 2.5 nM[1].
Chlormadinone acetate binds to the human androgen receptor in LNCaP cell cytosol with a Ki value of 3.8 nM[1].
Chlormadinone acetate binds to the human glucocorticoid receptor in IM-9 cell cytosol with a Ki value of 16 nM[1].

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

In Vivo

Chlormadinone acetate (5-45 μg/kg; p.o.; daily; for 5 consecutive days) exhibits dose-dependent progestomimetic activity in β-estradiol-pretreated rabbits. At an oral dose of 45 μg/kg, it significantly increases uterine weight and induces near-maximal endometrial transformation[1].
Chlormadinone acetate (4.64-21.5 mg/kg; p.o.; once daily; for 7 consecutive days) exhibits dose-dependent antiandrogenic activity in testosterone-treated castrated rats[1].
Chlormadinone acetate (21.5-100 mg/kg; p.o.; once daily; for 6 consecutive days) exhibits dose-dependent glucocorticoid activity in immature rats[1].

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

Animal Model: White New Zealand rabbits (female, ~1000 g, β-estradiol primed for cycle synchronization)[1]
Dosage: 5 μg/kg; 45 μg/kg
Administration: p.o.; daily; 5 days
Result: Induced a median histological endometrial transformation score of 1.42 and a relative uterus weight of 1.72 ± 0.52 g/1000 g body weight at 5 μg/kg.
Induced a median histological score of 1.92 and a statistically significant relative uterus weight of 2.67 ± 0.54 g/1000 g body weight, along with marked thickened uterine walls, endometrial hyperplasia with increased secretory glands, and a papillary surface epithelium pattern at 45 μg/kg.
Animal Model: Sprague-Dawley rats (male, 140-180 g, castrated, testosterone treated)[1]
Dosage: 4.64 mg/kg; 21.5 mg/kg
Administration: p.o.; daily; 7 days
Result: Caused an insignificant reduction in prostate weight, but significantly reduced seminal vesicle weights relative to testosterone-treated controls at both doses.
Reduced seminal vesicle weights by a maximum 40% at 21.5 mg/kg.
Reduced total accessory gland weights significantly at both doses relative to testosterone-treated controls, following the same pattern as seminal vesicle weights.
Animal Model: Wistar rats (male, immature, 50-70 g)[1]
Dosage: 21.5 mg/kg; 100 mg/kg
Administration: p.o.; daily; 6 days
Result: Reduced thymus weight at 21.5 mg/kg.
Caused a statistically significant 19% reduction in thymus weight relative to vehicle controls at 100 mg/kg.
Reduced adrenal gland weight significantly by 36% at the 100 mg/kg dose relative to vehicle controls.
Clinical Trial
Molecular Weight

404.93

Formula

C23H29ClO4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC([C@@]1(OC(C)=O)CC[C@@]2([H])[C@]3([H])C=C(Cl)C4=CC(CC[C@]4(C)[C@@]3([H])CC[C@]12C)=O)=O

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 : 10 mg/mL (24.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4696 mL 12.3478 mL 24.6956 mL
5 mM 0.4939 mL 2.4696 mL 4.9391 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 1 mg/mL (2.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (2.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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:

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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, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
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 2.4696 mL 12.3478 mL 24.6956 mL 61.7391 mL
5 mM 0.4939 mL 2.4696 mL 4.9391 mL 12.3478 mL
10 mM 0.2470 mL 1.2348 mL 2.4696 mL 6.1739 mL
15 mM 0.1646 mL 0.8232 mL 1.6464 mL 4.1159 mL
20 mM 0.1235 mL 0.6174 mL 1.2348 mL 3.0870 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Chlormadinone acetate
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HY-B1095
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