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TG 4-155

Names

[ CAS No. ]:
1164462-05-8

[ Name ]:
TG 4-155

[Synonym ]:
TG4-155
(E)-N-(2-(2-methyl-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide
N-(2-(2-methyl-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide

Biological Activity

[Description]:

TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM[1][2]. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1[1]. TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor[2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor
Research Areas >> Inflammation/Immunology
Research Areas >> Neurological Disease

[Target]

EP2 Receptor:9.9 nM (Ki)


[References]

[1]. Jiang J, et al. Role of prostaglandin receptor EP2 in the regulations of cancer cell proliferation, invasion, and inflammation. J Pharmacol Exp Ther. 2013 Feb;344(2):360-7.

[2]. Ganesh T. Prostanoid receptor EP2 as a therapeutic target. J Med Chem. 2014 Jun 12;57(11):4454-65.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H26N2O4

[ Molecular Weight ]:
394.46

[ Exact Mass ]:
394.18900

[ PSA ]:
61.72000

[ LogP ]:
4.19600

[ Storage condition ]:
2-8℃

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P280-P305 + P351 + P338-P337 + P313

[ RIDADR ]:
NONH for all modes of transport

Related Compounds