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