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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

GW 848687X

Cayman Chemical Item Number 10010410

(CAS 612831-24-0)

GW 848687X (CAS 612831-24-0)

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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 Gαq 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).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

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 Med Chem Lett 17 385-389 (2007).

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 441.9
Formulation A solution in methyl acetate
Purity ≥98%
Stability 1 year
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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FC1=CC=C(COC2=C(C3=C(C4=CC=CC(C(O)​=O)​=N4)​CCC3)​C=C(Cl)​C=C2)​C(F)​=C1

Background Reading

Stasch, J., Alonso-Alija, C., Apeler, H., et al. Pharmacological actions of a novel NO-independent guanylyl cyclase stimulator, BAY 41-8543: in vitro studies. Br J Pharmacol 135 333-343 (2002).

Stasch, J., Dembowsky, K., Perzborn, E., et al. Cardiovascular actions of a novel NO-independent guanylyl cyclase stimulator, BAY 41-8543: in vivo studies. Br J Pharmacol 135 344-355 (2002).

Evgenov, O.V., Kohane, D.S., Bloch, K.D., et al. Inhaled agonists of soluble guanylate cyclase induce selective pulmonary vasodilation. Am J Respir Crit Care Med 176 1138-1145 (2007).

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 Med Chem Lett 17 385-389 (2007).

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Size Price Quantity Subtotal
500 µg $65.00 $0.00
1 mg $124.00 $0.00
5 mg $520.00 $0.00
10 mg $910.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-02-12. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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