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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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5MG 72 Get Quote
10MG 115 Get Quote
25MG 237 Get Quote
50MG 380 Get Quote
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Biological Information

  • Product Name
    PF-02413873
  • Note
    Research use only, not for human use.
  • Brief Description
    PF-02413873 (PF-2413873) is a potent, selective, fully competitive, and orally active progesterone receptor (PR) antagonist with Ki of 9.7 nM.
  • Description
    PF-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.
  • In Vitro
    PF-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).
  • 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.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.
  • Synonyms
    PF-2413873
  • Pathway
    Nuclear Receptor/Transcription Factor
  • Target
    Progesterone Receptor
  • Recptor
    Progesterone Receptor
  • Research Area
    Other Indications
  • Indication
    Other Disease

Chemical Information

  • CAS Number
    936345-35-6
  • Formula Weight
    359.44
  • Molecular Formula
    C18H21N3O3S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (278.21 mM)
  • SMILES
    N#CC1=C(C)C=C(OC2=C(C)N(CS(=O)(C)=O)N=C2C3CC3)C=C1C
  • Chemical Name
    4-((3-cyclopropyl-5-methyl-1-((methylsulfonyl)methyl)-1H-pyrazol-4-yl)oxy)-2,6-dimethylbenzonitrile

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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.