Antagonist of the PGE2 receptor EP1
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GW 848687X

Item No. 10010410

Technical Information
Formal Name
6-[2-[5-chloro-2-[(2,4-digluorophenyl)methoxy]phenyl]-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid
CAS Number
612831-24-0
Molecular Formula
C24H18ClF2NO3
Formula Weight
Purity
≥98%
Formulation
A 5 mg/ml solution in methyl acetate
DMF: 5 mg/mlDMSO: 3 mg/mlEthanol: 10 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
282 nm
SMILES
FC1=CC=C(COC2=C(C3=C(C4=CC=CC(C(O)=O)=N4)CCC3)C=C(Cl)C=C2)C(F)=C1
InChi Code
InChI=1S/C24H18ClF2NO3/c25-15-8-10-23(31-13-14-7-9-16(26)12-20(14)27)19(11-15)17-3-1-4-18(17)21-5-2-6-22(28-21)24(29)30/h2,5-12H,1,3-4,13H2,(H,29,30)
InChi Key
PFODPHDNBFSMOX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).1 It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels.1 Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species.1 In a rat model of chronic inflammatory joint pain, GW 848687X shows complete anti-hyperalgesic activity with an ED50 value of 1.3 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Giblin, G.M.P., Bit, R.A., Brown, S.H., et alThe discovery of 6-[2-(5-chloro-2{[(2,4-difluorophenyl)-methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain. Bioorg. Med. Chem. Lett. 17, 385-389 (2007).