gpr132

NOX-6-18 (GPR132-B-160) is a highly potent and selective GPR132 antagonist with insulinotropic activity that modulates macrophage reprogramming in pancreatic islets and reduces weight gain.

ONC212 [a fluorinated-ONC201 analogue] is a selective GPR132 agonist.

Commendamide is a natural bacterial product that was discovered in a screen for commensal bacteria effector genes (Cbegs). Cbeg12 is a bacterial effector gene that encodes for its production. Commendamide is structurally similar to long-chain N-acyl-amides, which commonly signal, in mammals, through G protein-coupled receptors. Commendamide activates GPR132 (also known as G2A) with an EC50 value of 11.8 μM.

T-10418 is an agonist of the G2 accumulation protein (G2A), also known as G protein-coupled receptor GPR132, with an EC50 of 0.82 μM. It sensitizes primary sensory neurons in mice and demonstrates favorable pharmacokinetic properties in mouse models without significant toxicity at concentrations up to 100 μM.