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GW 848687X (CAS 612831-24-0) LS-H50

EP1 receptor antagonist
LS-H50-500 / 500 µg / $215
LS-H50-1000 / 1000 µg / $255
LS-H50-5000 / 5000 µg / $605
USA Shipment Only
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Description: Four G protein-coupled receptors, EP1-4, initiate cellular signaling in response to prostaglandin PGE2. The receptor EP1 acts via G alpha q to evoke diverse effects, including renal vasoconstriction, bronchoconstriction, hyperalgesia, allodynia, gastric protection, hyperthermia, and sleep inhibition. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM). 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 is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM). 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. 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. 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.

 

H50_ChemicalStructureImage.png
6-[2-[5-chloro-2-[(2,4-digluorophenyl)methoxy]phenyl]-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid
 
biochemical, chemical, antagonist
LS-H50
612831-24-0
C24H18ClF2NO3
≥98%
A solution in methyl acetate
 
FC1=CC=C(COC2=C(C3=C(C4=CC=CC(C(O)=O)=N4)CCC3)C=C(Cl)C=C2)C(F)=C1
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)
PFODPHDNBFSMOX-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 1 year shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: PTGER1 / EP1 related products

Usage Information

GW 848687X is supplied as a solution in methyl acetate. To change the solvent, simply evaporate the methyl acetate under a gentle stream of nitrogen and immediately add the solvent of choice. Solvents such as ethanol, DMSO, and dimethyl formamide purged with an inert gas can be used. The solubility of GW 848687X in these solvents is approximately 5 mg/ml. GW 848687X is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, GW 848687X should first be dissolved in ethanol and then diluted with the aqueous buffer of choice. GW 848687X has a solubility of approximately 0.25 mg/ml in a 1:3 solution of ethanol:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Giblin, G.M.P., Bit, R.A., Brown, S.H., et al. The 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. Medicinal Chem. Letters 17, 385-389 (2007).

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