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PF-02413873

Chemical Structure : PF-02413873

CAS No.: 936345-35-6

PF-02413873 (PF-2413873)

Catalog No.: PC-61896Not For Human Use, Lab Use Only.

PF-02413873 (PF-2413873) is a potent, selective, fully competitive, and orally active progesterone receptor (PR) antagonist with Ki of 9.7 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PF-02413873 (PF-2413873) is a potent, selective, fully competitive, and orally active progesterone receptor (PR) antagonist with Ki of 9.7 nM; displays >30-fold selectivity over other homologous nuclear hormone receptors, GR, AR, and MR; blocks the follicular phase increase in endometrial thickness, the midcycle lutenizing hormone surge, and elevation in estradiol in a dose-dependent fashion compared with placebo in clinical trials.

Other Indication

Phase 1 Discontinued

Physicochemical Properties

M.Wt 359.44
Formula C18H21N3O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((3-cyclopropyl-5-methyl-1-((methylsulfonyl)methyl)-1H-pyrazol-4-yl)oxy)-2,6-dimethylbenzonitrile

References

1. Bungay PJ, et al. Drug Metab Dispos. 2011 Aug;39(8):1396-405.

2. Howe DC, et al. J Pharmacol Exp Ther. 2011 Nov;339(2):642-53.

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