DAGL
Diacylglycerol lipase; DAG lipase; DGL
Diacylglycerol lipase (DAGL) is an enzyme that catalyzes the hydrolysis of diacylglycerol, releasing a free fatty acid and monoacylglycerol. DAGLα and DAGLβ have been identified as the enzymes predominantly responsible for the biosynthesis of the endogenous signaling lipid, 2-arachidonoylglycerol (2-AG). 2-AG is the most abundant endocannabinoid found in tissues and activates the CB1 and CB2 G-protein-coupled receptors. Endocannabinoid signaling via these receptors is involved in core body temperature control, inflammation, appetite promotion, memory formation, mood and anxiety regulation, pain relief, addiction reward, neuron protection, and more.
DAGL アイソフォーム特異的製品
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DAGL 関連製品 (14)
関連製品 (14)
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DAGL Isoform Comparison
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DO34
(DO34)
0 ImagesDO34 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.
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KT109
(KT109)
0 ImagesKT109 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.
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RHC 80267
(RHC 80267)
0 Images別名: U-57908RHC 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).
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KT172
0 ImagesKT172 is a DAGLβ inhibitor with an IC50 value of 11 nM. KT172 can be used for the research of metabolic and inflammatory.
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LEI-106
0 ImagesLEI-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.
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A1480LS
0 Images製品番号: HY-181482A1480LS 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.
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DO34 analog
0 ImagesDO34 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 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.
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DAGLβ-IN-1
0 ImagesDAGLβ-IN-1 is an inhibitor of diacylglycerol lipase-β (DAGLβ), serves as a versatile intermediate for the design of DAGL-tailored activity-based probes.
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L-Isoleucine orlistat
0 Images製品番号: HY-118340CAS 番号: 1072902-75-0L-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.
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DH-376
0 Images製品番号: HY-120171CAS 番号: 1848233-57-7DH-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.
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LEI105
0 Images製品番号: HY-112828CAS 番号: 1800327-36-9LEI105 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.
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RHC 80267 (Standard)
0 Images製品番号: HY-107416RCAS 番号: 83654-05-1別名: U-57908 (Standard)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).
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(R)-KT109
0 Images製品番号: HY-126031CAS 番号: 2055172-60-4(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.
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