439288-66-1
439288-66-1 structure
- Name: GW 627368
- Chemical Name: N-(benzenesulfonyl)-2-[4-(4,9-diethoxy-3-oxo-1H-benzo[f]isoindol-2-yl)phenyl]acetamide
- CAS Number: 439288-66-1
- Molecular Formula: C30H28N2O6S
- Molecular Weight: 544.618
- Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
- Create Date: 2017-03-23 15:50:11
- Modify Date: 2026-07-16 20:22:51
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GW627368(GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor(Ki= 100 nM) with additional human TP receptor affinity(Ki= 150 nM).IC50 value: Target: EP4 antagonistin vitro: At recombinant human prostanoid EP4 receptors expressed in HEK293 cells, GW627368X produced parallel rightward shifts of PGE2 concentration-effect (E/[A]) curves resulting in an affinity (pKb) estimate of 7.9 +/- 0.4. GW627368X appears to bind to human prostanoid TP receptors but not the TP receptors of other species. In human washed platelets, GW627368X (10 microM) produced 100% inhibition of U-46619 (EC100)-induced aggregation (approximate pA2 approximately 7.0) [1]. in vivo: 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 [2].
| Name | N-(benzenesulfonyl)-2-[4-(4,9-diethoxy-3-oxo-1H-benzo[f]isoindol-2-yl)phenyl]acetamide |
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| Synonyms |
inhibit,Inhibitor,Prostaglandin Rector,GW627368,GW 627368,GW-627368
GW627368, 10 mM in DMSO GW 627368X GW 627368;GW-627368;GW627368;GW-627368X;GW627368X;GW 627368X 4-(4,9-Diethoxy-1,3-dihydro-1-oxo-2H-benz[f]isoindol-2-yl)-N-(phenylsulfonyl)benzeneacetamide 2-(4-(4,9-Diethoxy-1-oxo-1H-benzo[f]isoindol-2(3H)-yl)phenyl)-N-(phenylsulfonyl)acetamide GW627368(GW627368X) GW-627368X unii-a9p1zgy0se Benzeneacetamide, 4-(4,9-diethoxy-1,3-dihydro-1-oxo-2H-benz[f]isoindol-2-yl)-N-(phenylsulfonyl) GW627368 N-(benzenesulfonyl)-2-(4-{4,9-diethoxy-1-oxo-1H,2H,3H-benzo[f]isoindol-2-yl}phenyl)acetamide 2-[4-(4,9-Diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]-N-(phenylsulfonyl)acetamide |
| Description | GW627368(GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor(Ki= 100 nM) with additional human TP receptor affinity(Ki= 150 nM).IC50 value: Target: EP4 antagonistin vitro: At recombinant human prostanoid EP4 receptors expressed in HEK293 cells, GW627368X produced parallel rightward shifts of PGE2 concentration-effect (E/[A]) curves resulting in an affinity (pKb) estimate of 7.9 +/- 0.4. GW627368X appears to bind to human prostanoid TP receptors but not the TP receptors of other species. In human washed platelets, GW627368X (10 microM) produced 100% inhibition of U-46619 (EC100)-induced aggregation (approximate pA2 approximately 7.0) [1]. in vivo: 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 [2]. |
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| Related Catalog | |
| References |
| Density | 1.3±0.1 g/cm3 |
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| Molecular Formula | C30H28N2O6S |
| Molecular Weight | 544.618 |
| Exact Mass | 544.166809 |
| PSA | 110.39000 |
| LogP | 4.95 |
| Index of Refraction | 1.645 |
| Storage condition | 2-8℃ |