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关于此项目
经验公式(希尔记法):
C30H28N2O6S
化学文摘社编号:
分子量:
544.62
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
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)
InChI key
XREWXJVMYAXCJV-UHFFFAOYSA-N
Biochem/physiol Actions
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
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable