GW627368X
GW627368X is a novel, potent and selective competitive antagonist of prostanoid EP4 receptors with additional human TP receptor affinity. Oral administration of GW627368X showed significant tumor regression characterized by tumor reduction and induction of apoptosis. Reduction in prostaglandin E2 synthesis also led to reduced level of VEGF in plasma. GW627368X will be a valuable tool to explore the role of the prostanoid EP4 receptor in many physiological and pathological settings.
1: Parida S, Parekh A, Dey G, Ghosh SC, Mandal M. Molecular inhibition of prostaglandin E2 with GW627368X: Therapeutic potential and preclinical safety assessment in mouse sarcoma model. Cancer Biol Ther. 2015;16(6):922-32. doi: 10.1080/15384047.2015.1040953. Epub 2015 Apr 20. PubMed PMID: 25894216.
2: Wilson RJ, Giblin GM, Roomans S, Rhodes SA, Cartwright KA, Shield VJ, Brown J, Wise A, Chowdhury J, Pritchard S, Coote J, Noel LS, Kenakin T, Burns-Kurtis CL, Morrison V, Gray DW, Giles H. 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. 2006 Jun;148(3):326-39. PubMed PMID: 16604093; PubMed Central PMCID: PMC1751567.
2: Wilson RJ, Giblin GM, Roomans S, Rhodes SA, Cartwright KA, Shield VJ, Brown J, Wise A, Chowdhury J, Pritchard S, Coote J, Noel LS, Kenakin T, Burns-Kurtis CL, Morrison V, Gray DW, Giles H. 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. 2006 Jun;148(3):326-39. PubMed PMID: 16604093; PubMed Central PMCID: PMC1751567.
| Chemical | |
|---|---|
| CAS Num | 439288-66-1 |
| Chemical Formula | C30H28N2O6S |
| Molecular Weight | 544.62 |
| IUPAC Chemical Name | 2-(4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl)-N-(phenylsulfonyl)acetamide |
| Exact Mass | 544.16681 |
| Elemental Analysis | C, 66.16; H, 5.18; N, 5.14; O, 17.63; S, 5.89 |
| Synonym | GW627368X; GW 627368X; GW-627368X; GW627368; GW 627368; GW-627368. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(NS(=O)(C1=CC=CC=C1)=O)CC2=CC=C(N(CC3=C4C(OCC)=C(C=CC=C5)C5=C3OCC)C4=O)C=C2 |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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