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TG6-10-1

Chemical Structure : TG6-10-1

CAS No.: 1415716-58-3

TG6-10-1 (EP2 antagonist)

Catalog No.: PC-45111Not For Human Use, Lab Use Only.

TG6-10-1 is a potent and selective antagonist of prostaglandin E2 receptor subtype EP2 with Kb of 17.8 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

TG6-10-1 is a potent and selective antagonist of prostaglandin E2 receptor subtype EP2 with Kb of 17.8 nM.
TG6-10-1 displays >300-fold selectivity over EP3, EP4, and IP receptors, 100-fold selectivity over EP1, 25-fold selectivity over FP and TP, and 10-fold selectivity over DP1 receptors.
TG6-10-1 completely recapitulates the effects of conditional ablation of COX-2 from principal forebrain neurons, accelerates recovery from weight loss, reduces brain inflammation, prevention of blood-brain barrier opening, and neuroprotection in the hippocampus, without modifying seizures acutely in the mouse pilocarpine model of SE.

Physicochemical Properties

M.Wt 448.4349
Formula C23H23F3N2O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Propenamide, N-[2-[2-(trifluoromethyl)-1H-indol-1-yl]ethyl]-3-(3,4,5-trimethoxyphenyl)-, (2E)-

References

1. Jiang J, et al. Proc Natl Acad Sci U S A. 2013 Feb 26;110(9):3591-6.

2. Rojas A, et al. Neuropharmacology. 2015 Jun;93:15-27.

3. Rojas A, et al. Neuropharmacology. 2016 Nov;110(Pt A):419-30.

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