2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. DAGL
  5. DAGL Inhibitor

DAGL Inhibitor

DAGL Isoform Comparison

DAGL Inhibitors (11):

Cat. No. Product Name Effect Purity
  • HY-117771
    DO34
    		Inhibitor 99.30%
    DO34 is a selective DAGL inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG. DO34 blocks de novo 2-AG synthesis, and suppresses tonic CB1 receptor activation. DO34 blocks depolarization-induced suppression of excitation and inhibition in the cerebellum and hippocampus. DO34 regulates feeding behavior and locomotor activity in mice. DO34 abolishes AM251-mediated enhancement of parallel fiber-evoked excitatory postsynaptic currents in cerebellar slices from MAGL global knockout mice. DO34 can be used for the research of energy balance disorder and neuroinflammation.
  • HY-107416
    RHC 80267
    		Inhibitor 99.41%
    RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).
  • HY-18541
    KT172
    		Inhibitor 99.5%
    KT172 is a DAGLβ inhibitor with an IC50 value of 11 nM. KT172 can be used for the research of metabolic and inflammatory.
  • HY-124314
    LEI-106
    		Inhibitor 99.9%
    LEI-106 is a dual ABHD6 and DAGL-α inhibitor, with a Ki of 0.8 μM for ABHD6, and an IC50 of 18 nM and a Ki of 0.7 μM for DAGL-α. LEI-106 blocks the synthesis of 2-arachidonoylglycerol, reduces the level of endothelial cell-derived 2-arachidonoylglycerol, without altering the levels of cannabinoids and diacylglycerol. LEI-106 is applicable to research related to diet-induced obesity and metabolic syndrome.
  • HY-118340
    L-Isoleucine orlistat
    		Inhibitor
    L-Isoleucine orlistat (Compound 15) is a diacylglycerol lipase α (DAGLα) inhibitor with an IC50 value of < 50 nM. L-Isoleucine orlistat is promising for research of neural signaling and inflammation-related diseases.
  • HY-181482
    A1480LS
    		Inhibitor
    A1480LS is a peripherally restricted, orally active covalent and irreversible inhibitor of DAGLα and DAGLβ, with IC50 values of 6 nM and 4 nM against human targets, respectively, and IC50 values ≤15 nM across mouse, rat, dog, monkey and human systems. A1480LS reduces the levels of 2-arachidonoylglycerol, arachidonic acid, and cyclooxygenase- and lipoxygenase-derived eicosanoids. A1480LS inhibits injury-induced production of 2-arachidonoylglycerol and arachidonic acid in the peripheral sciatic nerve, and suppresses the responses of high-threshold and wide-dynamic-range-like dorsal horn neurons to mechanical stimulation. A1480LS alleviates pain behaviors in rat models of inflammatory pain, neuropathic pain and chemotherapy-induced peripheral neuropathy.
  • HY-117771A
    DO34 analog
    		Inhibitor 98.42%
    DO34 analog is a structural analog of DO34 (HY-117771). DO34 is a selective DAGL inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG. DO34 can be used for the research of energy balance disorder and neuroinflammation.
  • HY-120171
    DH-376
    		Inhibitor
    DH-376 is a potent diacylglycerol lipase inhibitor with pIC50 values of 8.6 and 8.9 for ABHD6 and DAGLα, respectively. DH-376 prevents fasting-induced refeeding of mice. DH-376 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-112828
    LEI105
    		Inhibitor
    LEI105 is a potent, highly selective and reversible dual diacylglycerol lipase (DAGL)-α/DAGL-β inhibitor. LEI105 reduces 2-arachidonoylglycerol levels in Neuro2A cells. LEI105 also reduces cannabinoid CB1-receptor-mediated short-term synaptic plasticity in a mouse hippocampal slice model. LEI105 is promising for research of diseases, such as obesity, related metabolic disorders and neuroinflammation.
  • HY-107416R
    RHC 80267 (Standard)
    		Inhibitor
    RHC 80267 (Standard) is the analytical standard of RHC 80267 (HY-107416). This product is intended for research and analytical applications. RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).
  • HY-126031
    (R)-KT109
    		Inhibitor
    (R)-KT109 is a peripherally restricted serine hydrolase inhibitor that cannot cross the blood-brain barrier. (R)-KT109 irreversibly inhibits ABHD6, DAGLα and DAGLβ via carbamoylation of the active-site serine. (R)-KT109 exerts selective inhibitory effects on serine hydrolases in mouse brains, with pIC50 values of 8.6, 9.1 and 8.2 against human ABHD6, DAGLα and DAGLβ, respectively. (R)-KT109 effectively reduces the levels of 2-arachidonoylglycerol, arachidonic acid, eicosanoids and TNF-α. (R)-KT109 is widely used in studies of metabolic syndrome-related diseases and neuroinflammation.