
PF-02413873
CAS No. 936345-35-6
PF-02413873( PF-2413873 )
Catalog No. M16701 CAS No. 936345-35-6
PF-02413873 (PF-2413873) is a potent, selective, fully competitive, and orally active progesterone receptor (PR) antagonist with Ki of 9.7 nM.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 41 | Get Quote |
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5MG | 72 | Get Quote |
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10MG | 115 | Get Quote |
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25MG | 237 | Get Quote |
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50MG | 380 | Get Quote |
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100MG | 565 | Get Quote |
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500MG | 1215 | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NamePF-02413873
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NoteResearch use only, not for human use.
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Brief DescriptionPF-02413873 (PF-2413873) is a potent, selective, fully competitive, and orally active progesterone receptor (PR) antagonist with Ki of 9.7 nM.
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DescriptionPF-02413873 (PF-2413873) is a potent, selective, fully competitive, and orally active progesterone receptor (PR) antagonist with Ki of 9.7 nM; displays >30-fold selectivity over other homologous nuclear hormone receptors, GR, AR, and MR; blocks the follicular phase increase in endometrial thickness, the midcycle lutenizing hormone surge, and elevation in estradiol in a dose-dependent fashion compared with placebo in clinical trials.Other Indication Phase 1 Discontinued.
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In VitroPF-02413873 shows potent PR antagonist activity with a derived Ki of 9.7 nM in the T47D native functional assay.PF-02413873 (1 nM-10 μM) induces nuclear translocation only at high concentrations (>3 μM).
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In VivoPF-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.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). Animal Model:Cynomolgus macaques (3.7-5.7 kg; 5-6 years)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)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.
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SynonymsPF-2413873
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PathwayNuclear Receptor/Transcription Factor
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TargetProgesterone Receptor
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RecptorProgesterone Receptor
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Research AreaOther Indications
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IndicationOther Disease
Chemical Information
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CAS Number936345-35-6
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Formula Weight359.44
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Molecular FormulaC18H21N3O3S
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (278.21 mM)
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SMILESN#CC1=C(C)C=C(OC2=C(C)N(CS(=O)(C)=O)N=C2C3CC3)C=C1C
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Chemical Name4-((3-cyclopropyl-5-methyl-1-((methylsulfonyl)methyl)-1H-pyrazol-4-yl)oxy)-2,6-dimethylbenzonitrile
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Bungay PJ, et al. Drug Metab Dispos. 2011 Aug;39(8):1396-405.
2. Howe DC, et al. J Pharmacol Exp Ther. 2011 Nov;339(2):642-53.
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PF-02413873
PF-02413873 (PF-2413873) is a potent, selective, fully competitive, and orally active progesterone receptor (PR) antagonist with Ki of 9.7 nM.