2. Vitamin D Related/Nuclear Receptor
  3. Progesterone Receptor
  4. PF-02413873

PF-02413873  (Synonyms: PF-2413873)

Cat. No.: HY-11028 Purity: 99.29%
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PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo.

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

PF-02413873 Chemical Structure

PF-02413873 Chemical Structure

CAS No. : 936345-35-6

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10 mM * 1 mL in DMSO
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 USD 110 In-stock
Solution
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10 mg USD 160 In-stock
25 mg USD 320 In-stock
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Based on 1 publication(s) in Google Scholar

PF-02413873 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo[1][2].

IC50 & Target

Ki: 2.6 nM (progesterone receptor)[1]
In Vitro

PF-02413873 shows potent PR antagonist activity with a derived Ki of 9.7 nM in the T47D native functional assay[1].
PF-02413873 (1 nM-10 μM) induces nuclear translocation only at high concentrations (>3 μM)[1].

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

PF-02413873 Related Antibodies
In Vivo

PF-02413873 (2.5 and 10 mg/kg; p.o. twice daily for 10 days) induces a statistically significant reduction in endometrial thickness in cynomolgus macaques[1].
PF-02413873 (3 mg/kg; a single p.o.) exhibits t1/2 (4.2 h), Cmax (162 ng/mL) and CL/F (41 mL/min/kg)[1].

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

Animal Model: Cynomolgus macaques (3.7-5.7 kg; 5-6 years)[1]
Dosage: 2.5, 10 mg/kg
Administration: P.o. twice daily for 10 days
Result: Reduced the endometrial thickness of 43 and 56% at the dose of 2.5 and 10 mg/kg, respectively.
Animal Model: Cynomolgus macaques (3.7-5.7 kg; 5-6 years)[1]
Dosage: 3 mg/kg (Pharmacokinetic Analysis)
Administration: A single p.o.
Result: t1/2=4.2 h, Cmax=162 ng/mL, CL/F=41 mL/min/kg.
Clinical Trial
Molecular Weight

359.44

Formula

C18H21N3O3S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

N#CC1=C(C)C=C(OC2=C(C)N(CS(=O)(C)=O)N=C2C3CC3)C=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (278.21 mM; ultrasonic and warming and heat to 60°C; 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 2.7821 mL 13.9105 mL 27.8211 mL
5 mM 0.5564 mL 2.7821 mL 5.5642 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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: ≥ 1.25 mg/mL (3.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (3.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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, . 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

Purity: 99.29%

COA (251 KB) HNMR (136 KB) RP-HPLC (139 KB) LCMS (383 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7821 mL 13.9105 mL 27.8211 mL 69.5526 mL
5 mM 0.5564 mL 2.7821 mL 5.5642 mL 13.9105 mL
10 mM 0.2782 mL 1.3911 mL 2.7821 mL 6.9553 mL
15 mM 0.1855 mL 0.9274 mL 1.8547 mL 4.6368 mL
20 mM 0.1391 mL 0.6955 mL 1.3911 mL 3.4776 mL
25 mM 0.1113 mL 0.5564 mL 1.1128 mL 2.7821 mL
30 mM 0.0927 mL 0.4637 mL 0.9274 mL 2.3184 mL
40 mM 0.0696 mL 0.3478 mL 0.6955 mL 1.7388 mL
50 mM 0.0556 mL 0.2782 mL 0.5564 mL 1.3911 mL
60 mM 0.0464 mL 0.2318 mL 0.4637 mL 1.1592 mL
80 mM 0.0348 mL 0.1739 mL 0.3478 mL 0.8694 mL
100 mM 0.0278 mL 0.1391 mL 0.2782 mL 0.6955 mL
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PF-02413873 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:

PF-02413873936345-35-6PF-2413873PF02413873PF 02413873PF2413873PF 2413873Progesterone ReceptorNR3C3nonsteroidalprogesteronePRnucleartranslocationendometrialInhibitorinhibitorinhibit

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