TG6-10-1|EP2 inhibitor|DC Chemicals

TG6-10-1|EP2 inhibitor|DC Chemicals

TG6-10-1 is a cell-permeable,highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, Kb = 17.8 nM).

Product Name: TG6-10-1 |Catalog Number:  DC8348 | cas: 1415716-58-3 | Other names:  | Chemical name：(E)-N-(2-(2-(trifluoromethyl)-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide | Molecule Formula: C23H23F3N2O4 | MW: 448.43

A cell-permeable, 3-acryl-acrylamide derivative that acts as a highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, Kb = 17.8 nM). Exhibits about 300-fold selectivity for the EP2 receptor over human EP3, EP4, and IP receptors, about 100- fold selectivity over human EP1, 25-fold selectivity against human FP and TP, and 10-fold selectivity against human DP1 receptors. Does not affect the activity of about 40 enzymes, ion channels, receptors, and neurotransmitters even at higher concentrations (˜10 µM). Shown to significantly reduce the induction of several inflammatory cytokines and chemokines and reduces the opening of blood-brain barrier during neuronal inflammation. Displays good pharmacokinetic properties with a half-life of 1.6 h and brain to plasma ratio of 1.6 in a murine model (5 mg/kg i.p.).

For research and scientific purpose only, not for human use.