KT-109 (KT109) is a potent, selective inhibitor of DAGLβ with IC50 of 42 nM, displays about 60-fold selectivity over DAGLα.
KT-109 shows negligible activity against other key enzymes involved in endocannabinoid signaling, including FAAH, MAGL and ABHD11.
KT-109 disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids in mouse peritoneal macrophages.
KT-109 reverses nociceptive behaviour in mouse models of inflammatory and neuropathic pain; possesses one remaining off-target ABHD6 (IC50=16 nM).
