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About This Item
Empirical Formula (Hill Notation):
C18H21N3O3S
CAS Number:
Molecular Weight:
359.44
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Product Name
PF-02413873, ≥98% (HPLC)
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
SMILES string
CC1=C(C#N)C(C)=CC(OC2=C(C)N(CS(=O)(C)=O)N=C2C3CC3)=C1
InChI key
QSFGZNVRVZHUGV-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
room temp
Quality Level
Biochem/physiol Actions
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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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