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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
37 Results for "
Lipase MAGL
" in MedChemExpress (MCE) Product Catalog:
Products (37)
37 Results for "Lipase MAGL" in MCE Product Catalog:
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6 Publications Verification
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MJN110 is an orally active and selective monoacylglycerol lipase (MAGL) inhibitor with IC50s of 9.1 nM and 2.1 nM for hMAGL and 2-arachidonoylglycerol (2-AG), respectively . MJN110 produces opioid-sparing effects and displays strong antihyperalgesic activity .
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4 Cited Publications
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JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibitor with IC50s of 2 and 4 nM, respectively .
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3 Cited Publications
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JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
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Elcubragistat (ABX-1431) is a highly effective, selective, orally active, and blood-brain barrier-permeable monoacylglycerol lipase (MAGL) inhibitor, with an IC50 value of 14 nM .
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2 Cited Publications
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JJKK 048 is a highly selective and potent monoacylglycerol lipase (MAGL) inhibitor with IC50 values of 214 pM, 275 pM and 363 pM for human, rat, and mouse MAGL. JJKK 048 displays low cross-reactivity with other endocannabinoid targets. JJKK 048 can be used in the research of diseases such as cancer, neurodegenerative diseases, and pain .
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CAY10499 (MAGL-IN-5) is a non-selective lipase inhibitor with IC50 values of 144 nM and 14 nM for monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), respectively. Additionally, CAY10499 exhibits anti-inflammatory and antiviral activities .
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1 Cited Publications
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JNJ-42226314, a chemical probe, is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain .
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1 Cited Publications
MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays .
Synonyms: 7-HCA; Umbelliferyl Arachidonate; 7-HC-arachidonate
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7-Hydroxycoumarinyl arachidonate (7-HCA) is a fluorogenic substrate of cytosolic phospholipase A2 (PLA2). 7-Hydroxycoumarinyl arachidonate is also a fluorogenic substrate for monoacylglycerol lipase (MAGL). MAGL protein catalyzes the hydrolysis of 7-Hydroxycoumarinyl arachidonat to generate Arachidonic acid (AA) and the highly fluorescent 7-hydroxyl coumarin (7-HC; HY-N0573). Release of 7-HC can be measured using a fluorometer .
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MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain .
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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 .
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N-Arachidonyl maleimide is a potent, irreversible inhibitor of monoacylglycerol lipase (MAGL) with an IC50 value of 140 nM .
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FAAH/MAGL-IN-4 (Compound 13) is a potent fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) inhibitor with IC50s of 9.1 nM and 7.9 μM, respectively. FAAH/MAGL-IN-4 can be used for the research of pain and CNS disorders .
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JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC50 of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research .
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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 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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CAY10762 is an inhibitor of monoacylglycerol lipase (MAGL; IC50=34.1 nM). It reduces hydrogen peroxide-induced lactate dehydrogenase (LDH) release from Neuro2a cells when used at a concentration of 1 μM. CAY10762 (10 mg/kg) increases levels of 2-arachidonoyl glycerol in mouse brain.
Cat. No.: HY-150702
CAS No.: 2361575-20-2
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MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease .
Cat. No.: HY-168032
CAS No.: 3036792-74-9
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MAGL-IN-18 (compound 118) is a potent Monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 0.03 nM .
Cat. No.: HY-146342
CAS No.: 2848719-34-4
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FAAH/MAGL-IN-3 (Compound 10) is an irreversible fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) dual inhibitor with IC50 values of 179 and 759 nM against FAAH and MAGL, respectively. FAAH/MAGL-IN-3 shows low PAMPA (Parallel Artificial Membrane Permeability Assay) permeability .
Cat. No.: HY-116143
CAS No.: 1352011-38-1
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SAR127303 is an orally active, selective, competitive monoacylglycerol lipase (MAGL) covalent inhibitor with IC50s of 3.8 nM and 29 nM for mouse and human MAGL, respectively. SAR127303 potently elevates hippocampal levels of 2-AG in mice. SAR127303 decreased long term potentiation (LTP) of CA1 synaptic transmission and acetylcholine release in the hippocampus. SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. SAR127303 slows down epileptogenesis .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
