| Identification | Back Directory | [Name]
PF-2413873 | [CAS]
936345-35-6 | [Synonyms]
PF-2413873
4-[3-cyclopropyl-5-methyl-1-(methylsulfonylmethyl)pyrazol-4-yl]oxy-2,6-dimethylbenzonitrile
4-((3-cyclopropyl-5-methyl-1-((methylsulfonyl)methyl)-1H-pyrazol-4-yl)oxy)-2,6-dimethylbenzonitrile
nonsteroidal,inhibit,PF 2413873,Progesterone Receptor,endometrial,PF-2413873,nuclear,PF 02413873,NR3C3,PF2413873,PF-02413873,translocation,progesterone,Inhibitor | [Molecular Formula]
C18H21N3O3S | [MDL Number]
MFCD16987601 | [MOL File]
936345-35-6.mol | [Molecular Weight]
359.44 |
| Chemical Properties | Back Directory | [Melting point ]
163-164 °C | [Boiling point ]
548.9±50.0 °C(Predicted) | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
DMSO : 100 mg/mL (278.21 mM; Need ultrasonic) | [form ]
Solid | [pka]
1.12±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo[1][2]. | [Biological Activity]
PF-02413873 is a potentselective and fully competitive non-steroidal progesterone receptor (PR) antagonist th at blocks progesterone binding and PR nuclear translocation. PF-02413873 suppresses endometrial growth in the macaque and human. | [in vivo]
PF-02413873 (2.5 and 10 mg/kg; p.o. twice daily for 10 days) induces a statistically significant reduction in endometrial thickness in cynomolgus macaques[1].
PF-02413873 (3 mg/kg; a single p.o.) exhibits t1/2 (4.2 h), Cmax (162 ng/mL) and CL/F (41 mL/min/kg)[1]. | Animal Model: | Cynomolgus macaques (3.7-5.7 kg; 5-6 years)[1] | | Dosage: | 2.5, 10 mg/kg | | Administration: | P.o. twice daily for 10 days | | Result: | Reduced the endometrial thickness of 43 and 56% at the dose of 2.5 and 10 mg/kg, respectively. |
| Animal Model: | Cynomolgus macaques (3.7-5.7 kg; 5-6 years)[1] | | Dosage: | 3 mg/kg (Pharmacokinetic Analysis) | | Administration: | A single p.o. | | Result: | t1/2=4.2 h, Cmax=162 ng/mL, CL/F=41 mL/min/kg. |
| [References]
[1] Howe DC, et, al. The translational efficacy of a nonsteroidal progesterone receptor antagonist, 4-[3-cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy,-2,6-dimethylbenzonitrile (PF-02413873), on endometrial growth in macaque and human. J Pharmacol Exp Ther. 2011 Nov;339(2):642-53. DOI:10.1124/jpet.111.183848
[2] Bungay PJ, et, al. Preclinical and clinical pharmacokinetics of PF-02413873, a nonsteroidal progesterone receptor antagonist. Drug Metab Dispos. 2011 Aug;39(8):1396-405. DOI:10.1124/dmd.110.037234 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|