GW 627368X CAS: 439288-66-1
MF: C30H28N2O6S
MW: 544.62
A selective and potent competitive antagonist of the EP4 receptor.

GW 627368X (CAS 439288-66-1)

GW 627368X | CAS 439288-66-1 is rated 5.0 out of 5 by 1.
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Synonym: 4-(4,9-diethoxy-1,3-dihydro-1-oxo-2H-benz[f]isoindol-2-yl)-N-(phenylsulfonyl)-benzeneacetamide
Application: A selective and potent competitive antagonist of the EP4 receptor
CAS Number: 439288-66-1
Purity: >96%
Molecular Weight: 544.62
Molecular Formula: C30H28N2O6S
* Refer to Certificate of Analysis for lot specific data (including water content).
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GW 627368X is a selective and potent 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. 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. The effects of prostaglandin E2 (PGE2) are transduced by at least four different receptors designated EP1, EP2, EP3, and EP4.


References

1 Coleman, R.A., Smith, W.L., 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).

Physical State :
Solid
Solubility :
Soluble in water (0.3 mg/ml at 25.0° C), DMSO (~10 mg/ml), DMF (~30 mg/ml), and 1: 1 DMF: PBS (pH 7.2) (~0.3 mg/ml).
Storage :
Store at -20° C
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.65 (Predicted)
Ki Data :
EP4: Ki= 100 nM (human); TP: Ki= 158 nM (human)
pK Values :
pKa: 5.25 (Predicted), pKb: 3.52 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5312130
MDL Number :
MFCD12912327
SMILES :
CCOC1=C2CN(C(=O)C2=C(C3=CC=CC=C31)OCC)C4=CC=C(C=C4)CC(=O)NS(=O)(=O)C5=CC=CC=C5

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Certificate of Analysis

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GW 627368X  Product Citations

See how others have used GW 627368X. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 29466417  El Moussawi, L.|Chakkour, M.|Kreydiyyeh, SI.| et al. 2018. PLoS ONE. 13: e0193139.

PMID: # 27806992  Laan, LC. et al. 2017. FASEB J. 31: 719-731.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Paul et al Paul et al. (PubMed ID 23523954) found that the EP4 antagonist, GW 627368X, had a significant antiproliferative effect in Kaposi's sarcoma-associated herpesvirus and Epstein-Barr virus associated non-Hodgkin lymphoma cell lines. -SCBT Publication Review
Date published: 2015-07-07
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