TG6-10-1

TG6-10-1 is a potent antagonist of E prostanoid receptor 2 (EP₂; K_b = 17.8 nM in C6 glioma cells overexpressing human EP₂).¹ It is 300-, 25-, and 10-fold selective for EP₂ over other prostanoid receptors, including human EP_3-4, 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.^1,2

WARNING This product is not for human or veterinary use.

1. Jiang, J., Quan, Y., Ganesh, T., et al. Inhibition of the prostaglandin receptor EP₂ following status epilepticus reduces delayed mortality and brain inflammation. Proc. Natl. Acad. Sci. USA 110(9), 3591-3596 (2013).

2. Rojas, A., Ganesh, T., Lelutiu, N., et al. Inhibition of the prostaglandin EP₂ receptor is neuroprotective and accelerates functional recovery in a rat model of organophosphorus induced status epilepticus. Neuropharmacology 93, 15-27 (2015).

Matsumoto, N., Singh, N., Lee, K.S., et al. The epoxy fatty acid pathway enhances cAMP in mammalian cells through multiple mechanisms. Prostaglandins Other Lipid Mediat. 162, 106662 (2022).