Arrestin-3/β-Arrestin 2 Activator

IHCH-7113 is a 5-HT2AR agonist with EC₅₀ values of 58.9 nM (Gq bioluminescence resonance energy transfer assay) and 44.7 nM (β-arrestin 2 bioluminescence resonance energy transfer assay). IHCH-7113 activates both Gαq-mediated signaling pathways and β-arrestin 2 recruitment pathways. IHCH-7113 is applicable for research related to depression.

Tyr-c [D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 is a multi-opioid receptor (Opioid Receptor) modulator, acting as a MOR/KOR agonist and a DOR antagonist. Tyr-c [D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 activates the G protein-mediated cAMP inhibitory pathway and β-arrestin2 recruitment pathway downstream of MOR, with an EC₅₀ of 159 nM for β-arrestin2 recruitment, an EC₅₀ of 1.1 nM for MOR-mediated calcium mobilization, and an EC₅₀ of 397 nM for KOR. Tyr-c [D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 exhibits potent analgesic activity in vivo. It can be used in studies related to opioid receptor function and analgesia.

BMS-986331 is an orally active selective N-Formyl Peptide Receptor 2 (FPR2) agonist with an EC₅₀ of 0.5 nM in humans and 1 nM in rats. BMS-986331 activates Gαi2, GαoA, Gα12, Gα13 signaling pathways, recruits β-arrestin1 and β-arrestin2, and inhibits downstream cAMP. BMS-986331 induces the expression and release of the pro-resolution cytokine IL-10. BMS-986331 improves cardiac structure and function in a rat model of heart failure induced by permanent coronary artery occlusion. BMS-986331 can be used for the research of heart failure.