MedChemExpress - Model PF-02413873 -936345-35-6
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].MCE products for research use only. We do not sell to patients.
PF-02413873
MCE China：PF-02413873
Brand：MedChemExpress (MCE)
Cat. No.HY-11028
CAS：936345-35-6
Synonyms：PF-2413873
Purity：99.29%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping：Room temperature in continental US; may vary elsewhere.
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.
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].
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].
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. 0 --> PF-02413873 Related Antibodies
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References：
[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 Exp Ther. 2011 Nov;339(2):642-53. [Content Brief]
[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. [Content Brief]
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