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dagl

" in MedChemExpress (MCE) Product Catalog:

15

Inhibitors & Agonists

1

Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18540
    KT109
    1 Publications Verification

    		 MAGL DAGL Metabolic Disease Inflammation/Immunology
    KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC50 of 42 nM. KT109 has ~60-fold selectivity for DAGLβ over DAGLα. KT109 shows inhibitory activity against PLA2G7 (IC50=1 µM). KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 (cPLA2 or PLA2G4A). KT109 perturbs a lipid network involved in macrophage inflammatory responses and lowers 2-Arachidonoylglycerol (HY-W011051), Arachidonic acid (HY-109590) and eicosanoids in mouse peritoneal macrophages .
    KT109
  • HY-117771
    DO34
    5 Publications Verification

    		 DAGL Neurological Disease Metabolic Disease
    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 .
    DO34
  • HY-107416
    RHC 80267

    U-57908

    		 DAGL Acyltransferase mAChR COX Phospholipase Neurological Disease Metabolic Disease
    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) .
    RHC 80267
  • HY-18541
    KT172

    		DAGL Metabolic Disease Inflammation/Immunology
    KT172 is a DAGLβ inhibitor with an IC50 value of 11 nM. KT172 can be used for the research of metabolic and inflammatory .
    KT172
  • HY-124314
    LEI-106

    		MAGL DAGL Metabolic Disease
    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 .
    LEI-106
  • HY-120851
    O-7460

    		Cannabinoid Receptor DAGL Metabolic Disease
    O-7460 is a potent and selective DAGLα inhibitor, with an IC50 of 0.69 μM. O-7460 shows selectivity over onoacylglycerol lipase (MAGL), human CB1 and CB2 cannabinoid receptors. O-7460 can decrease HFD-caused an up-regulation of 2-AG levels .
    O-7460
  • HY-120171
    DH-376

    		DAGL MAGL Metabolic Disease
    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.
    DH-376
  • HY-18551
    DAGLβ-IN-1

    		DAGL Inflammation/Immunology
    DAGLβ-IN-1 is an inhibitor of diacylglycerol lipase-β (DAGLβ), serves as a versatile intermediate for the design of DAGL-tailored activity-based probes .
    DAGLβ-IN-1
  • HY-117771A
    DO34 analog

    		DAGL Neurological Disease Metabolic Disease
    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 .
    DO34 analog
  • HY-126031
    (R)-KT109

    		DAGL Inflammation/Immunology
    (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 .
    (R)-KT109
  • HY-112828
    LEI105

    		DAGL Neurological Disease Metabolic Disease Inflammation/Immunology
    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 .
    LEI105
  • HY-126031A
    (S)-KT109

    		Endogenous Metabolite Others
    (S)-KT109 is an inhibitor of diacylglycerol lipase β (DAGLβ) with low inhibitory activity (IC50 = 39.81 nM). (S)-KT109 has relatively low inhibitory activity against DAGLα-mediated hydrolysis of 1-stearoyl-2-arachidonoyl-sn-glycerol (IC50 = 794.3 nM). (S)-KT109 also has relatively low inhibitory activity against α/β-amidase domain-containing 6 (ABHD6) (IC50 = 630.9 nM) .
    (S)-KT109
  • HY-118340
    L-Isoleucine orlistat

    		DAGL Inflammation/Immunology
    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 .
    L-Isoleucine orlistat
  • HY-181482
    A1480LS

    		DAGL Neurological Disease
    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 .
    A1480LS
  • HY-107416R
    RHC 80267 (Standard)

    U-57908 (Standard)

    		 DAGL Reference Standards Acyltransferase mAChR COX Phospholipase Neurological Disease Metabolic Disease
    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) .
    RHC 80267 (Standard)

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