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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Progesterone Receptor-PF-02413873
PF-02413873

Chemical Structure : PF-02413873

CAS No.: 936345-35-6

PF-02413873 (PF-2413873, PF 02413873)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PF-02413873 (PF-2413873) is a potent, selective, fully competitive, and orally active progesterone receptor (PR) antagonist with Ki of 9.7 nM.
PF-02413873 displays >30-fold selectivity over other homologous nuclear hormone receptors, GR, AR, and MR.
PF-02413873 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.

物理化学性质&存储条件

分子量 359.44
分子式 C18H21N3O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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

参考文献

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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