LY237 is a potent GPR84 full agonist, with EC 50 values of 0.189 nM and 0.07 nM in cAMP inhibition assay and calcium flux assay, respectively. LY237 binds to the amphipathic orthosteric pocket of GPR84, stabilizes the active conformation of the receptor, and promotes its coupling with Gαi protein. LY237 can be used in research related to ulcerative colitis, fibrotic diseases, non-alcoholic steatohepatitis, and acute respiratory distress syndrome [1] [2].
In Vitro, LY237 interacts with specific residues in the extracellular loop 2 and transmembrane domain of the receptor, thereby driving activation signal transduction[2].
References:
[1]. Ieremias L, et al. Minimal Structural Variation of GPR84 Full Agonist Causes Functional Switch to Inverse Agonism. Journal of medicinal chemistry. 2025 Apr 24;68(8):7973-8009.
[2]. Liu H, et al. Structural insights into ligand recognition and activation of the medium-chain fatty acid-sensing receptor GPR84. Nature communications. 2023 Jun 06;14(1):3271.
In Vitro, LY237 interacts with specific residues in the extracellular loop 2 and transmembrane domain of the receptor, thereby driving activation signal transduction[2].
References:
[1]. Ieremias L, et al. Minimal Structural Variation of GPR84 Full Agonist Causes Functional Switch to Inverse Agonism. Journal of medicinal chemistry. 2025 Apr 24;68(8):7973-8009.
[2]. Liu H, et al. Structural insights into ligand recognition and activation of the medium-chain fatty acid-sensing receptor GPR84. Nature communications. 2023 Jun 06;14(1):3271.