GW 627368X
GW 627368X Basic information
- Product Name:
- GW 627368X
- Synonyms:
-
- GW 627368X
- GW 627368
- 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-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]-N-(phenylsulfonyl)acetamide
- GW 627368;GW-627368;GW627368;GW-627368X;GW627368X;GW 627368X
- CS-1654
- GW627368(GW627368X)
- N-(benzenesulfonyl)-2-[4-(4,9-diethoxy-3-oxo-1H-benzo[f]isoindol-2-yl)phenyl]acetamide
- CAS:
- 439288-66-1
- MF:
- C30H28N2O6S
- MW:
- 544.62
- Product Categories:
-
- Inhibitors
- Mol File:
- 439288-66-1.mol
GW 627368X Chemical Properties
- 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
GW 627368X Usage And Synthesis
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-
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
GW 627368XSupplier
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- sales@boylechem.com
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- 021-58950125
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- 021-58955995
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- 021-52996696，15000506266 15000506266
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