ChemicalBook--->CAS DataBase List--->439288-66-1

439288-66-1

439288-66-1 Structure

439288-66-1 Structure
IdentificationBack Directory
[Name]

GW 627368X
[CAS]

439288-66-1
[Synonyms]

CS-1654
GW 627368
GW 627368X
GW627368(GW627368X)
GW 627368;GW-627368;GW627368;GW-627368X;GW627368X;GW 627368X
N-(benzenesulfonyl)-2-[4-(4,9-diethoxy-3-oxo-1H-benzo[f]isoindol-2-yl)phenyl]acetamide
2-(4-(4,9-Diethoxy-1-oxo-1H-benzo[f]isoindol-2(3H)-yl)phenyl)-N-(phenylsulfonyl)acetamide
4-(4,9-Diethoxy-1,3-dihydro-1-oxo-2H-benz[f]isoindol-2-yl)-N-(phenylsulfonyl)benzeneacetamide
Benzeneacetamide, 4-(4,9-diethoxy-1,3-dihydro-1-oxo-2H-benz[f]isoindol-2-yl)-N-(phenylsulfonyl)-
2-[4-(4,9-Diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]-N-(phenylsulfonyl)acetamide
[Molecular Formula]

C30H28N2O6S
[MDL Number]

MFCD12912327
[MOL File]

439288-66-1.mol
[Molecular Weight]

544.62
Chemical PropertiesBack Directory
[density ]

1.327±0.06 g/cm3(Predicted)
[storage temp. ]

Sealed in dry,Store in freezer, under -20°C
[solubility ]

DMSO : 100 mg/mL (183.61 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
[form ]

Powder
[pka]

5.25±0.10(Predicted)
[color ]

White to off-white
[InChIKey]

XREWXJVMYAXCJV-UHFFFAOYSA-N
[SMILES]

O=C(CC1=CC=C(C=C1)N(C2=O)CC3=C2C(OCC)=C4C=CC=CC4=C3OCC)NS(=O)(C5=CC=CC=C5)=O
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
[WGK Germany ]

WGK 3
[Storage Class]

11 - Combustible Solids
Hazard InformationBack Directory
[Description]

The effects of prostaglandin E2 (PGE2) are transduced by at least four distinct receptors designated EP1, EP2, EP3, and EP4. 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. 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.
[Uses]

GW 627368 is a selective EP4 receptor competitive antagonist.
[in vivo]

GW627368 (GW627368X) (0-15 mg/kg; p.o.; every alternate day for 28 days) shows significant tumor regression characterized by tumor reduction and induction of apoptosis[3].

Animal Model:6-8 weeks Swiss albino mice[3]
Dosage:0 mg/kg, 5 mg/kg, 10 mg/kg, 15 mg/kg, 15 mg/kg
Administration:Oral administration, every alternate day for 28 days
Result:Displayed anti-tumor and anti-proliferative potential in sarcoma 180 bearing mice.
[IC 50]

EP
[References]

[1] RICHARD J WILSON. 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[J]. British Journal of Pharmacology, 2009, 148 3: 326-339. DOI: 10.1038/sj.bjp.0706726
Spectrum DetailBack Directory
[Spectrum Detail]

GW 627368X(439288-66-1)1HNMR
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