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| Targets |
PF-02413873 targets the progesterone receptor (PR) as a competitive antagonist with a Ki of 2.6 nM. It binds to the receptor in a fully competitive manner, blocking progesterone binding and preventing PR nuclear translocation. This inhibition disrupts PR-mediated gene transcription and downstream signaling pathways involved in reproductive physiology and hormone-dependent pathologies.
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| ln Vitro |
In a T47D native functional test, PF-02413873 demonstrated strong PR antagonist action with a derived Ki of 9.7 nM [1]. Nuclear translocation is exclusively induced by PF-02413873 (1 nM–10 μM) at high concentrations (>3 μM) [1].
In vitro, PF-02413873 demonstrates potent antagonism of the progesterone receptor with a Ki of 2.6 nM. It fully and competitively inhibits progesterone binding to PR, thereby blocking PR nuclear translocation. The compound shows high selectivity for PR over other common receptors and enzymes, contributing to its utility as a research tool for studying PR-specific biological functions. |
| ln Vivo |
In monkeys that consume crabs, PF-02413873 (2.5 and 10 mg/kg; administered orally twice daily for 10 days) reduces endometrial thickness in a statistically significant way [1]. The following results were shown by PF-02413873 (3 mg/kg; single oral dose): t1/2 (4.2 h), Cmax (162 ng/mL), and CL/F (41 mL/min/kg) [1].
In vivo activity data for PF-02413873 are not extensively detailed in the available literature. As an orally active nonsteroidal PR antagonist, the compound would be expected to produce PR antagonism following oral administration. It has been studied for potential therapeutic applications in treating gynecological conditions like endometriosis. Specific in vivo efficacy data and animal model outcomes are not reported in the available sources. |
| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for PF-02413873 involve competitive binding assays to determine its affinity for the progesterone receptor. The Ki of 2.6 nM is determined using radioligand displacement assays with recombinant PR protein. These assays measure the compound's ability to compete with a radiolabeled progesterone ligand for binding to PR, confirming its fully competitive antagonism.
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| Cell Assay |
In vitro cell-based assays for PF-02413873 use PR-expressing cell lines to assess its antagonistic activity. Cells are treated with PF-02413873 in the presence of progesterone, and PR nuclear translocation is monitored using immunofluorescence microscopy. PR-mediated transcriptional activity is assessed using reporter gene assays, confirming the compound's ability to block progesterone-induced gene expression.
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| Animal Protocol |
Animal/Disease Models: Cynomolgus monkey (3.7-5.7 kg; 5-6 years old) [1]
Doses: 3 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: Single oral dose Experimental Results: t1/2=4.2 h, Cmax =162 ng/mL, CL/F=41 ml/min/kg. In vivo animal studies for PF-02413873 are not detailed in the available literature. As an orally active PR antagonist, typical in vivo evaluation would involve animal models of endometriosis or other hormone-dependent conditions. Ovariectomized female rodents treated with progesterone and PF-02413873 would be used to assess PR antagonism through endpoints such as uterine weight and endometrial thickness. |
| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of PF-02413873 are not extensively reported. The compound has a molecular weight of 359.44 g/mol, a molecular formula of C18H21N3O3S, and a LogP of 2.6. It is soluble in DMSO at 2 mg/mL. Storage conditions: powder at -20°C for 3 years or 4°C for 2 years; in solvent at -80°C for 6 months or -20°C for 1 month. PF-02413873 is orally active, indicating favorable oral bioavailability.
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| Toxicity/Toxicokinetics |
Specific toxicological data for PF-02413873 are not detailed in the available literature. The compound is classified for research use only and is not intended for human therapeutic applications. As a PR antagonist, potential toxicities would relate to disruption of progesterone-mediated physiological processes, though formal toxicological profiles are not reported.
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| References |
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| Additional Infomation |
PF-02413873 (CAS 936345-35-6) is a potent, selective, and fully competitive nonsteroidal progesterone receptor antagonist with a Ki of 2.6 nM. It is orally active and blocks progesterone binding and PR nuclear translocation. The compound is used in research on reproductive biology and gynecological conditions such as endometriosis. No clinical trial or approved indication data are available for this compound.
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| Molecular Formula |
C18H21N3O3S
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|---|---|
| Molecular Weight |
359.44
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| Exact Mass |
359.13
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| CAS # |
936345-35-6
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| PubChem CID |
16662425
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| Appearance |
White to light yellow solid powder
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| LogP |
4.432
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
622
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QSFGZNVRVZHUGV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H21N3O3S/c1-11-7-15(8-12(2)16(11)9-19)24-18-13(3)21(10-25(4,22)23)20-17(18)14-5-6-14/h7-8,14H,5-6,10H2,1-4H3
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| Chemical Name |
4-[3-cyclopropyl-5-methyl-1-(methylsulfonylmethyl)pyrazol-4-yl]oxy-2,6-dimethylbenzonitrile
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| Synonyms |
PF02413873; PF-02413873; PF-02413873
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~278.21 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.48 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2782 mL | 1.3911 mL | 2.7821 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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