GW 627368X

Cayman Chemical Item Number 10009162

(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
InCHI Code
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​1S/C30H28N2O6S/c1-3-37-28-23-12-8-9-13-24(23)​29(38-4-2)​27-25(28)​19-32(30(27)​34)​21-16-14-20(15-17-21)​18-26(33)​31-39(35,36)​22-10-6-5-7-11-22/h5-17H,3-4,18-19H2,1-2H3,(H,31,33)​
InCHI Key
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XREWXJVMYAXCJV-UHFFFAOYSA-N

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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
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Pricing updated 2015-05-24. Prices are subject to change without notice.

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Cayman Chemical Company regularly evaluates our shipping methods to ensure product stability is maintained and our corporate environmental impact is minimized. Products selected for review are evaluated and shipping methods are certified by our Scientists. While occasionally our method of shipping a product may change, rest assured the shipping conditions on all Cayman Chemical products have been reviewed and validated.

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Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.

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Ann Arbor, Michigan 48108 USA

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