2. Vitamin D Related/Nuclear Receptor
  3. Progesterone Receptor
  4. Tanaproget

Tanaproget is an orally effective, selective nonsteroidal progesterone receptor (PR) agonist targeting human PR with an IC50 of 1.7 nM. Tanaproget promotes the interaction between PR receptors and coactivators (such as SRC-1), thereby inhibiting the secretion of matrix metalloproteinases (MMP-3/MMP-7) and reducing endometrial tissue invasion and angiogenesis. Tanaproget can be used for contraception and endometriosis inhibition research.

For research use only. We do not sell to patients.

Tanaproget Chemical Structure

Tanaproget Chemical Structure

CAS No. : 304853-42-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Tanaproget Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Tanaproget

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tanaproget is an orally effective, selective nonsteroidal progesterone receptor (PR) agonist targeting human PR with an IC50 of 1.7 nM. Tanaproget promotes the interaction between PR receptors and coactivators (such as SRC-1), thereby inhibiting the secretion of matrix metalloproteinases (MMP-3/MMP-7) and reducing endometrial tissue invasion and angiogenesis. Tanaproget can be used for contraception and endometriosis inhibition research[1][2][3].

Cellular Effect
Cell Line Type Value Description References
T47D IC50
0.5 nM
Compound: 8
Displacement of [3H]R5020 from human PR in human T47D cells by whole cell assay
Displacement of [3H]R5020 from human PR in human T47D cells by whole cell assay
[PMID: 18318463]
In Vitro

Tanaproget (1 nM; 3-5 days) significantly down-regulated pro-MMP-3 expression in endometrial stromal cells isolated from normal women, even under IL-1α stimulation[1].
Tanaproget (1-100 pM; 48-72 h) inhibited the secretion of pro-MMP-3 and pro-MMP-7 in endometrial organ cultures from exogenous endometriosis patients[1].
Tanaproget (0.1 nM; 24 h) induced alkaline phosphatase activity in T47D cells with an EC50 of 0.15 nM (human), which is comparable to steroidal progestins[2].

Tanaproget against PR of different species with IC50s of 1.7 nM (human), 0.3 nM (monkey), and 0.5 nM (rat, rabbit)[2].

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

Tanaproget Related Antibodies

Western Blot Analysis[1]

Cell Line: Human endometrial stromal cells (normal and endometriosis patients)
Concentration: 1-500 nM (natural progesterone), 1-100 pM (synthetic progestins including Tanaproget)
Incubation Time: 3-5 d
Result: Suppressed pro-MMP-3 expression in normal stromal cells, even after IL-1α challenge.
Reduced pro-MMP-3 and pro-MMP-7 secretion compared to placebo.

Cell Viability Assay[2]

Cell Line: T47D breast carcinoma cells
Concentration: 0.001–100 nM
Incubation Time: 24 h
Result: Induced alkaline phosphatase activity with an EC50 of 0.15 nM, demonstrating full agonist activity comparable to medroxyprogesterone acetate (MPA) and trimegestone (TMG).
In Vivo

Tanaproget (300 μg/kg; gavage/sustained-release capsules; once daily; 14-16 days) significantly reduces the number and size of human endometriotic lesions in the ncr/nude mouse endometriosis model[1].

Tanaproget (0.03 mg/kg; oral; once daily; 4 days) completely inhibits ovulation in the Sprague-Dawley rat ovulation inhibition model and is 30 times more potent than steroidal progestins[2].

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

Animal Model: Human endometriosis xenograft model in ncr/nude athymic mice (female, 5-week-old, ovariectomized)[1]
Dosage: 300μg/kg (2% Tween 80/0.5% methylcellulose)
Administration: Gavage or slow-release capsule, daily for 14–16 days
Result: Reduced the number and size of human endometrial lesions derived from endometriosis patients, with complete regression in 33% of treated mice.
Animal Model: Sprague-Dawley rats (female, 200 g, estrus-synchronized)[2]
Dosage: 0.03 mg/kg (corn oil)
Administration: Oral gavage, daily for 4 days
Result: Completely inhibited ovulation in all treated rats at 0.03 mg/kg, showing 30-fold higher efficacy than medroxyprogesterone acetate (MPA).
Molecular Weight

297.37

Formula

C16H15N3OS
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

N#CC1=CC=C(C2=CC=C(NC(OC3(C)C)=S)C3=C2)N1C
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 (168.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3628 mL 16.8141 mL 33.6281 mL
5 mM 0.6726 mL 3.3628 mL 6.7256 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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:
%
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% 
+
%
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 3.3628 mL 16.8141 mL 33.6281 mL 84.0704 mL
5 mM 0.6726 mL 3.3628 mL 6.7256 mL 16.8141 mL
10 mM 0.3363 mL 1.6814 mL 3.3628 mL 8.4070 mL
15 mM 0.2242 mL 1.1209 mL 2.2419 mL 5.6047 mL
20 mM 0.1681 mL 0.8407 mL 1.6814 mL 4.2035 mL
25 mM 0.1345 mL 0.6726 mL 1.3451 mL 3.3628 mL
30 mM 0.1121 mL 0.5605 mL 1.1209 mL 2.8023 mL
40 mM 0.0841 mL 0.4204 mL 0.8407 mL 2.1018 mL
50 mM 0.0673 mL 0.3363 mL 0.6726 mL 1.6814 mL
60 mM 0.0560 mL 0.2802 mL 0.5605 mL 1.4012 mL
80 mM 0.0420 mL 0.2102 mL 0.4204 mL 1.0509 mL
100 mM 0.0336 mL 0.1681 mL 0.3363 mL 0.8407 mL
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Tanaproget Related Classifications

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.

Keywords:

Tanaproget304853-42-7NSP-989NSP989NSP 989Progesterone ReceptorNR3C3Inhibitorinhibitorinhibit

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