Home Tools

PF-02413873

Catalog No. T28362 CAS 936345-35-6

Synonyms: PF02413873

PF-02413873 is a competitive antagonist of nonsteroidal Progesterone Receptor with a Ki of 2.6 nM. PF-02413873 can be used in studies about the treatment of gynecological conditions such as endometriosis.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PF-02413873, CAS 936345-35-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 46.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 128.00
25 mg	In stock	$ 263.00
50 mg	In stock	$ 422.00
100 mg	In stock	$ 628.00
500 mg	In stock	$ 1,350.00
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

Bulk Inquiry

Select Batch

Purity: 100%

Purity: 99.90%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PF-02413873 is a competitive antagonist of nonsteroidal progesterone receptor with a Ki of 2.6 nM. PF-02413873 can be used in studies about the treatment of gynecological conditions such as endometriosis.
Targets&IC50	Progesterone receptor:2.6 nM (Ki)
In vitro	PF-02413873 induces nuclear translocation only at high concentrations (>3 μM). PF-02413873 shows a derived Ki of 9.7 nM in the T47D native functional assay[3].
In vivo	In cynomolgus macaques, PF-02413873 (3 mg/kg; p.o.) exhibits a t1/2 of 4.2 h, a Cmax of 162 ng/mL and CL/F of 41 mL/min/kg. PF-02413873 (2.5 and 10 mg/kg; p.o.) reduces the endometrial thickness of 43 and 56%, respectively[3].

Synonyms	PF02413873
Molecular Weight	359.44
Formula	C18H21N3O3S
CAS No.	936345-35-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

DMSO: 95 mg/mL (264.30 mM), ultrasonic and warming and heat to 60°C

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Bungay PJ, et, al. Preclinical and clinical pharmacokinetics of PF-02413873, a nonsteroidal progesterone receptor antagonist. Drug Metab Dispos. 2011 Aug;39(8):1396-405. 2. Jones HM, et al. Application of PBPK modelling in drug discovery and development at Pfizer. Xenobiotica. 2012 Jan;42(1):94-106. 3. Howe DC, et, al. The translational efficacy of a nonsteroidal progesterone receptor antagonist, 4-[3-cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy,-2,6-dimethylbenzonitrile (PF-02413873), on endometrial growth in macaque and human. J Pharmacol Exp Ther. 2011 Nov;339(2):642-53.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Bioactive Compounds Library Max Inhibitor Library Bioactive Compound Library ReFRAME Related Library Clinical Compound Library Orally Active Compound Library

Related Products

Related compounds with same targets

U-46619 Cridanimod Desogestrel Nomegestrol acetate Ulipristal Progesterone Levonorgestrel Benzonitrile, 4-[[5-cyclopropyl-3-methyl-1-[(methylsulfonyl)methyl]-1H-pyrazol-4-yl]oxy]-2,6-dimethyl-

Dose Conversion

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

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

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.

Keywords

PF-02413873 936345-35-6 Others Progesterone Receptor nonsteroidal inhibit PF 2413873 PF02413873 endometrial PF-2413873 nuclear PF 02413873 NR3C3 PF2413873 translocation progesterone Inhibitor inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.