MilliporeSigma™ Calbiochem™ Prostaglandin EP2 Receptor Antagonist, TG6-10-1

Description

• A cell-permeable, 3-acryl-acrylamide derivative that acts as a highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, K b = 17.8nM)
• 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 (˜10μM)
• 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 (5mg/kg i.p.).