For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I008649 |
| CAS Number | 936345-35-6 |
| Synonyms | 4-[3-cyclopropyl-5-methyl-1-(methylsulfonylmethyl)pyrazol-4-yl]oxy-2,6-dimethylbenzonitrile |
| Molecular Formula | C18H21N3O3S |
| Purity | ≥95% |
| InChI | 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 |
| InChIKey | QSFGZNVRVZHUGV-UHFFFAOYSA-N |
| SMILES | CC1=CC(=CC(=C1C#N)C)OC2=C(N(N=C2C3CC3)CS(=O)(=O)C)C |
| Reference | [1]. 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 [2]. 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. |
