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    PF-04418948
    PF-04418948

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1881
    CAS #: 1078166-57-0Purity ≥98%

    Description: PF-04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist. PF-04418948 inhibited prostaglandin E2(PGE2-induced increase in cAMP in cells expressing EP2 receptors with a functional KB value of 1.8 nM. In human myometrium, PF-04418948 produced a parallel, rightward shift of the butaprost-induced inhibition of the contractions induced by electrical field stimulation with an apparent KB of 5.4 nM. In dog bronchiole and mouse trachea, PF-04418948 produced parallel rightward shifts of the PGE2-induced relaxation curve with a KB of 2.5 nM and an apparent KB of 1.3 nM respectively. Reversal of the PGE2-induced relaxation in the mouse trachea by PF-04418948 produced an IC50 value of 2.7 nM. 

    References: Br J Pharmacol. 2011 Dec;164(7):1847-56; Br J Pharmacol. 2013 Jan;168(1):129-38.

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    Molecular Weight (MW)409.41 
    FormulaC23H20FNO5 
    CAS No.1078166-57-0 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 81 mg/mL (197.8 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: 1-(4-Fluorobenzoyl)-3-[[(6-methoxy-2-naphthalenyl)oxy]methyl]-3-azetidinecarboxylic acid
    InChi Key: LWJGMYMNSNVCEM-UHFFFAOYSA-N
    InChi Code: InChI=1S/C23H20FNO5/c1-29-19-8-4-17-11-20(9-5-16(17)10-19)30-14-23(22(27)28)12-25(13-23)21(26)15-2-6-18(24)7-3-15/h2-11H,12-14H2,1H3,(H,27,28)
    SMILES Code: O=C(C1(COC2=CC=C3C=C(OC)C=CC3=C2)CN(C(C4=CC=C(C=C4)F)=O)C1)O
    SynonymsPF04418948; PF-04418948; PF 04418948; PF4418948; PF-4418948; PF 4418948.


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    In Vitro

    In vitro activity: PF-04418948 antagonizes the effects of butaprost and PGE2 on an EFS-induced contraction of the human myometrium, and antagonizes PGE2-induced relaxation of carbachol pre-contracted rings of mouse trachea. PF-04418948 competitively inhibits relaxations of murine and guinea pig trachea induced by ONO-AE1-259 and PGE2 respectively. PF-04418948 restores neutrophil extracellular traps (NETs) formation in neutrophils isolated from BMT mice or HSCT patients.


    Kinase Assay: PF-04418948 is an orally active, potent and selective prostaglandin EP2 receptor antagonist with an IC50 of 16 nM.

    In VivoIn Rats, PF-04418948 (10 mg/kg, p.o.) reduces the mean cutaneous blood flow peak response and AUC0–60 by 41% and 61%, respectively. 
    Animal modelSprague Dawley rats 
    Formulation & DosageFormulated in 0.5% w/v methylcellulose + 0.1% v/v Tween 80 in purified water; 10 mg/kg; p.o.
    ReferencesBr J Pharmacol. 2011 Dec;164(7):1847-56; Br J Pharmacol. 2013 Jan;168(1):129-38. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    PF-04418948


    EP2 receptor-driven responses: relaxation of isolated mouse tracheal tissue.

    PF-04418948

    EP1 receptor-mediated responses: contraction of guinea pig isolated tracheal tissue.  2013 Jan;168(1):129-38.

     PF-04418948


    EP2 receptor-driven responses: relaxation of guinea pig isolated tracheal tissue.

    PF-04418948

    EP3 receptor-mediated responses: depolarization of guinea pig isolated vagal tissue.

     


    PF-04418948

    EP4 receptor-mediated responses: relaxation of rat and human isolated tracheal tissue.  2013 Jan;168(1):129-38.


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