1. GPCR/G Protein
  2. Prostaglandin Receptor

PF-04418948 

Cat. No.: HY-18966 Purity: 99.60%
Handling Instructions

PF-04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist with IC50 of 16 nM, displays >2000-fold functional selectivity for the human EP2 receptor over antagonist activity against the human EP1, EP3, EP4, DP1 and CRTH2 receptors.

For research use only. We do not sell to patients.

PF-04418948 Chemical Structure

PF-04418948 Chemical Structure

CAS No. : 1078166-57-0

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 440 In-stock
Estimated Time of Arrival: December 31
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Customer Review

    PF-04418948 purchased from MCE. Usage Cited in: J Virol. 2018 Aug 1. pii: JVI.01018-18.

    A549 cells are added with an EP2 or an EP4 inhibitor. After 48 h, cells are subjected to WB with an anti-Axl antibody.
    • Biological Activity

    • Technical Information

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    • References

    Description

    PF-04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist with IC50 of 16 nM, displays >2000-fold functional selectivity for the human EP2 receptor over antagonist activity against the human EP1, EP3, EP4, DP1 and CRTH2 receptors. IC50 value: 16 nM Target: EP2 in vitro: PF-04418948 inhibits 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. [1] in vivo: 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. Given orally, PF-04418948 attenuated the butaprost-induced cutaneous blood flow response in rats. [1] PF-04418948 competitively inhibits relaxations of murine and guinea pig trachea induced by ONO-AE1-259 and PGE2 respectively.[2]

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4425 mL 12.2127 mL 24.4254 mL
    5 mM 0.4885 mL 2.4425 mL 4.8851 mL
    10 mM 0.2443 mL 1.2213 mL 2.4425 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Molecular Weight

    409.41

    Formula

    C₂₃H₂₀FNO₅

    CAS No.

    1078166-57-0

    SMILES

    O=C(C1(COC2=CC=C3C=C(OC)C=CC3=C2)CN(C(C4=CC=C(F)C=C4)=O)C1)O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.60%

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    Product Name:
    PF-04418948
    Cat. No.:
    HY-18966
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    PF-04418948

    Cat. No.: HY-18966