An orally active, potent, selective EP2 receptor antagonist
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PF-04418948

Item No. 15016

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(4-fluorobenzoyl)-3-[[(6-methoxy-2-naphthalenyl)oxy]methyl]-3-azetidinecarboxylic acid
CAS Number
1078166-57-0
Molecular Formula
C23H20FNO5
Formula Weight
409.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 16 mg/mlEthanol: 0.5 mg/ml
λmax
230 nm
SMILES
O=C(O)C1(COC2=CC(C=CC(OC)=C3)=C3C=C2)CN(C(C4=CC=C(F)C=C4)=O)C1
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)
InChi Key
LWJGMYMNSNVCEM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $108

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    10 mg

    $161

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    50 mg

    $748

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    100 mg

    $1,061

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    Product Description

    PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).1 It is over a thousand-fold less active at other prostanoid receptors, including other EP receptors. PF-04418948 can be used in cells and tissues.2,3 In rats, it significantly reduces the effects of the EP2-selective agonist butaprost on cutaneous blood flow when given orally.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. af Forselles, K.J., Root, J., Clarke, T., et al. In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP2 receptor antagonist. Br. J. Pharmacol. 164(7), 1847-1856 (2011).

    2. Birrell, M.A., Maher, S.A., Buckley, J., et al. Selectivity profiling of the novel EP2 receptor antagonist, PF-04418948, in functional bioassay systems: Atypical affinity at the guinea pig EP2 receptor. Br. J. Pharmacol. 168, 129-138 (2013).

    3. Säfholm, J., Dahlén, S.E., Delin, I., et al. PGE2 maintains the tone of the guinea pig trachea through a balance between activation of contractile EP1 receptors and relaxant EP2 receptors. Br. J. Pharmacol. 168(4), 794-806 (2013).