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HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis[1].

[1] Zhao C, et al. Biased allosteric activation of ketone body receptor HCAR2 suppresses inflammation. Mol Cell. 2023 Sep 7;83(17):3171-3187.e7. DOI:10.1016/j.molcel.2023.07.030