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Documenti fondamentali

SML3414

Sigma-Aldrich

GW627368X

≥98% (HPLC)

Sinonimo/i:

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, GW 627368, GW 627368X, GW-627368, GW-627368X, GW627368

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About This Item

Formula empirica (notazione di Hill):
C30H28N2O6S
Numero CAS:
Peso molecolare:
544.62
Numero MDL:
Codice UNSPSC:
12352200
NACRES:
NA.77

Livello qualitativo

Saggio

≥98% (HPLC)

Stato

powder

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

2-8°C

Stringa SMILE

O=C(CC1=CC=C(C=C1)N(C2=O)CC3=C2C(OCC)=C4C=CC=CC4=C3OCC)NS(=O)(C5=CC=CC=C5)=O

InChI

1S/C30H28N2O6S/c1-3-37-28-23-12-8-9-13-24(23)29(38-4-2)27-25(28)19-32(30(27)34)21-16-14-20(15-17-21)18-26(33)31-39(35,36)22-10-6-5-7-11-22/h5-17H,3-4,18-19H2,1-2H3,(H,31,33)
XREWXJVMYAXCJV-UHFFFAOYSA-N

Azioni biochim/fisiol

GW627368X is a potent and selective prostaglandin E2 receptor EP4 antagonist with additional affinity for thromboxane A2 receptor (pKi = 7.0/EP4, 6.8/TP, <5.3/DP, EP1, EP2, EP3, FP & IP) that effectively reduces basal (non-detectable at 0.1 nM with COX inhibition or pIC50 = 6.3 without) and PGE2-stimulated cAMP (pKb = 7.9) in human EP4-expressing HEK293 cells. GW627368X inhibits EP4-, but not EP2-, induced tissue relaxation (pKb = 9.2; precontracted piglet & rabbit saphenous vein), but not TP agonist U46619-elevated tissue tone (pKb <5) ex vivo, and blocks PGE2-enhanced HBV virus replication in mice in vivo (1 mg/kg/day i.p.) by preventing CD8 + T-cell impairment by PGE2
Potent and selective prostaglandin E2 (PGE2) receptor EP4 antagonist in vitro and in vivo

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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J F Hiken et al.
Oncogene, 36(16), 2319-2327 (2016-11-22)
Approximately 75% of breast cancers express estrogen receptor α (ERα) and depend on estrogen signals for continued growth. Aromatase inhibitors (AIs) prevent estrogen production and inhibit ER signaling, resulting in decreased cancer recurrence and mortality. Advanced tumors treated with AIs
Tomomi Ohmura et al.
Molecular biology of the cell, 28(12), 1622-1635 (2017-04-22)
The role of prostaglandin A2 (PGA2) in modulation of vascular endothelial function is unknown. We investigated effects of PGA2 on pulmonary endothelial cell (EC) permeability and inflammatory activation and identified a receptor mediating these effects. PGA2 enhanced the EC barrier

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