PF-02413873

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-02413873 (PF-2413873) 是一种有效、选择性、完全竞争性、口服活性的孕酮受体 (PR) 拮抗剂，Ki 为 9.7 nM。

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.

PF-02413873 shows potent PR antagonist activity with a derived Ki of 9.7 nM in the T47D native functional assay.PF-02413873 (1 nM-10 μM) induces nuclear translocation only at high concentrations (>3 μM).

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.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). Animal Model:Cynomolgus macaques (3.7-5.7 kg; 5-6 years)Dosage:2.5, 10 mg/kg Administration:P.o. twice daily for 10 days Result:Reduced the endometrial thickness of 43 and 56% at the dose of 2.5 and 10 mg/kg, respectively.Animal Model:Cynomolgus macaques (3.7-5.7 kg; 5-6 years)Dosage:3 mg/kg (Pharmacokinetic Analysis)Administration:A single p.o.Result:t1/2=4.2 h, Cmax=162 ng/mL, CL/F=41 mL/min/kg.

PF-2413873

Nuclear Receptor/Transcription Factor

Progesterone Receptor

Progesterone Receptor

Other Indications

Other Disease

936345-35-6

359.44

C18H21N3O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (278.21 mM)

N#CC1=C(C)C=C(OC2=C(C)N(CS(=O)(C)=O)N=C2C3CC3)C=C1C

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

(-20℃)

With Ice Pack

≥ 2 years