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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
room temp
SMILES字符串
CC1=C(C#N)C(C)=CC(OC2=C(C)N(CS(=O)(C)=O)N=C2C3CC3)=C1
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
InChI key
QSFGZNVRVZHUGV-UHFFFAOYSA-N
生化/生理作用
PF-02413873 is a potent, selective and fully competitive non-steroidal progesterone receptor (PR) antagonist that blocks progesterone binding and PR nuclear translocation. PF-02413873 suppresses endometrial growth in the macaque and human.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
Peter J Bungay et al.
Drug metabolism and disposition: the biological fate of chemicals, 39(8), 1396-1405 (2011-05-06)
The recently discovered selective nonsteroidal progesterone receptor (PR) antagonist 4-[3-cyclopropyl-1-(methylsulfonylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy-2,6-dimethylbenzonitrile (PF-02413873) was characterized in metabolism studies in vitro, in preclinical pharmacokinetics in rat and dog, and in an initial pharmacokinetic study in human volunteers. Clearance (CL) of PF-02413873 was found
David C Howe et al.
The Journal of pharmacology and experimental therapeutics, 339(2), 642-653 (2011-08-19)
There is considerable ongoing investment in the research and development of selective progesterone receptor (PR) modulators for the treatment of gynecological conditions such as endometriosis. Here, we provide the first report on the clinical evaluation of a nonsteroidal progesterone receptor
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