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You are here:Home-Inhibitors & Agonists-Metabolic Enzyme/Protease-Diacylglycerol Lipase (DAGL)

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DGAT (acyl-CoA: diacylglycerol acyltransferase) is a transmembrane enzyme that acts in the final and committed step of triacylglycerides (TAGs) synthesis, and it has been proposed to be the rate-limiting enzyme in plant storage lipid accumulation. DGAT catalyzes the acylation of sn-1,2-diacylglycerol (DAG) at the sn-3 position using an acyl-CoA substrate. DGAT has been proposed to be the rate-limiting enzyme in plant storage lipid accumulation. DGAT is considered a key enzyme for biotechnological purposes; it might be utilized to increase oil content in oleaginous plant species.

DGAT1 and DGAT2 are two of the enzymes that are responsible for the main part of TAG synthesis in most organisms, and they have been studied in many eukaryotic organisms.

Cat. No. Product Name CAS No. Information
H5063

DO-34

 		1848233-58-8

DO-34 is a highly potent dual DAGLα/β inhibitor with IC50 of 6 nM 3-8 nM, respectively; shows excellent selectivity for DAGLs with the only detectable serine hydrolase off-targets being ABHD6 and PLA2G7; significantly decreases whole brain levels of 2-AG, anandamide, and arachidonic acid in the mouse LPS inflammatory pain model.
H5062

DH-376

 		1848233-57-7

DH-376 is a highly potent dual DAGLα/β inhibitor with IC50 of 6 nM and 3-8 nM, respectively; shows excellent selectivity for DAGLs with the only detectable serine hydrolase off-targets being ABHD6 (pIC50=7.0) and PLA2G7; significantly decreases whole brain levels of 2-AG, anandamide, and arachidonic acid in the mouse LPS inflammatory pain model.
H5066

LEI-105

 		1800327-36-9

LEI-105 is a potent, highly selective, and reversible dual DAGL-α/DAGL-β inhibitor with pIC50 pf 7.5/7.4 respectively; shows no activity against other enzymes involved in endocannabinoid metabolism (ABHD6, ABHD12, MAGL, or FAAH), and no affinity for CB1 receptor; concentration-dependently reduces 2-AG levels, but not anandamide levels, in Neuro2A cells; reduces cannabinoid CB1-receptor-mediated short-term synaptic plasticity in a mouse hippocampal slice model.
H5065

KT-172

 		1402612-56-9

KT-172 is a potent, selective inhibitor of DAGLβ with IC50 of 60 nM; displays selectivity over DAGLα, and negligible activity against other key enzymes involved in endocannabinoid signaling, including FAAH, MAGL, and ABHD11; disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids in mouse peritoneal macrophages; possesses one remaining off-target ABHD6 (IC50=5 nM).
H5064

KT-109

 		1402612-55-8

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

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