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PZ0367

Sigma-Aldrich

PF-02413873

≥98% (HPLC)

Synonym(s):

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

Empirical Formula (Hill Notation):
C18H21N3O3S
CAS Number:
936345-35-6
Molecular Weight:
359.44
MDL number:
MFCD16987601
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

room temp

SMILES string

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

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_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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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