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GW 627368X Exclusive

Cayman Chemical Item Number 10009162

(CAS 439288-66-1)

GW 627368X (CAS 439288-66-1)

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Description

The effects of prostaglandin E2 (PGE2) are transduced by at least four distinct receptors designated EP1, EP2, EP3, and EP4.1 GW 627368X is a potent and selective competitive antagonist of the EP4 receptor with additional human TP receptor affinity. In competition radioligand bioassays, GW 627368X had affinity for human EP4 and TP receptors with Ki values of 100 nM and 158 nM, respectively.2 Affinity for all other human prostanoid receptors is >5.0 µM. In human washed platelets, GW 627368X produced 100% inhibition of U-46619 (EC100)-induced aggregation at a concentration of 10 µM.

1 Coleman, R.A., Smith, W.L., and Narumiya, S. Classification of prostanoid receptors: Properties, distribution, and structure of the receptors and their subtypes. Pharmacol Rev 46 205-229 (1994).

2 Wilson, R.J., Giblin, G.M.P., Roomans, S., et al. GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): A novel, potent and selective prostanoid EP4 receptor antagonist. Br J Pharmacol 148 326-339 (2006).

Formal Name 4-​(4,​9-​diethoxy-​1,​3-​dihydro-​1-​oxo-​2H-​benz[f]isoindol-​2-​yl)-​N-​(phenylsulfonyl)-​benzeneacetamide
CAS Number 439288-66-1
Molecular Formula C30H28N2O6S
Formula Weight 544.6
Formulation A crystalline solid
Purity ≥96%
λmax 217, 229, 248, 295, 353 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CCOc1c2C(=O)​N(Cc2c(OCC)​c2ccccc12)​c1ccc(cc1)​CC(=O)​NS(=O)​(=O)​c1ccccc1

Background Reading

Wilson, R.J., Giblin, G.M.P., Roomans, S., et al. GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): A novel, potent and selective prostanoid EP4 receptor antagonist. Br J Pharmacol 148 326-339 (2006).

Coleman, R.A., Smith, W.L., and Narumiya, S. Classification of prostanoid receptors: Properties, distribution, and structure of the receptors and their subtypes. Pharmacol Rev 46 205-229 (1994).

GW 627368X is available in the following screening library:

Size Price Quantity Subtotal
1 mg $46.00 $0.00
5 mg $207.00 $0.00
10 mg $368.00 $0.00
25 mg $805.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-05-25. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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