产品描述:
TG6-10-1 is a potent antagonist of E prostanoid receptor 2 (EP2; Kb = 17.8 nM in C6 glioma cells overexpressing human EP2).{40354} It is 300-, 25-, and 10-fold selective for EP2 over other prostanoid receptors, including human EP3-4, FP and TP, and DP1 receptors, respectively. TG6-10-1 is also selective for EP2 over a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s >10 μM). In vivo, TG6-10-1 increases survival, decreases weight loss, prevents induction of IL-1β, IL-6, TNF-α, and MCP-1/CCL2 mRNA, and inhibits neuronal cell death in the hippocampus in mouse and rat models of status epilepticus induced by pilocarpine (Item No. 14487) and diisopropyl fluorophosphate, respectively.{40354,40355}