TG4-155 |
رقم الكتالوجGC13732 |
TG4-155 هو مناهض لمستقبلات EP2 قوي ودائم وانتقائي مع Ki يبلغ 9.9 نانومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1164462-05-8
Sample solution is provided at 25 µL, 10mM.
IC50: 2.4 nM for KB EP2; 11.4 nM for KB EP4
TG4-155 is a brain penetrant EP2 antagonist.
Prostaglandin E2 (PGE2) evokes distinct responses via four different ‘E prostanoid’ (EP) receptors. EP2, a G protein-coupled receptor, has diverse roles, such as those in cancer, inflammation, and neuroprotection.
In vitro: Using a set of cell-based TR-FRET assays of cAMP formation, a previous study screened a small molecule library and identified TG4-155 and TG4-166 as the most potent ones. TG4-155 and TG4-166 also showed robust inhibition of PGE2 -induced cAMP accumulation in human EP2-overexpressing C6 glioma cells, without affecting prostaglandin EP4 or β2-adrenergic receptors. Both TG4-155 and TG4-166 could cause a robust rightward shift in the PGE2 dose–response curve without affecting the maximal response to PGE2. TG4-155 at 1 μM caused 1,120-fold shift and TG4-166 at 1 μM caused a 651-fold shift in the PGE2 EC50 [1].
In vivo: TG4-155 could significantly reduced neuronal injury in hippocampus when administered in mice beginning 1 h after termination of pilocarpine-induced status epilepticus. The salutary actions of TG4-155 raised the possibility that selective block of EP2 signaling through small molecules can be an innovative therapeutic strategy for inflammation-related brain injury [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Jiang, J. ,Ganesh, T.,Du, Y., et al. Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E2 receptor subtype EP2. Proceedings of the National Academy of Sciences of the United States of America 109(8), 3149-3154 (2012).
Average Rating: 5
(Based on Reviews and 7 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *