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Merck
CN

PZ0367

Sigma-Aldrich

PF-02413873

≥98% (HPLC)

别名:

4-[3-Cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy-2,6-dimethylbenzonitrile, 4-[[3-Cyclopropyl-5-methyl-1-[(methylsulfonyl)methyl]-1H-pyrazol-4-yl]oxy]-2,6-dimethyl-benzonitrile, PF 2413873, PF-2413873

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About This Item

经验公式(希尔记法):
C18H21N3O3S
分子量:
359.44
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

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:

分析证书(COA)

Lot/Batch Number

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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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