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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
24 Results for "
Endocannabinoid Inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (24)
24 Results for "Endocannabinoid Inhibitors" in MCE Product Catalog:
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3 Cited Publications
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LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .
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2 Cited Publications
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AM404, an inhibitor of endocannabinoid reuptake, blocks anandamide transport with IC50 values in the low micromolar range . AM404 is able to relax rat isolated hepatic arteries contracted with Phenylephrine, with a pEC50 value of 7.4 (corresponding to an EC50 of 0.04 μM). Neuroprotective Effect .
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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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Category:
Alkaloids Other Alkaloids Endogenous metabolite Disease Research Fields Inflammation/Immunology
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1
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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Triterpenes Terpenoids Euphorbiaceae Plants Disease Research Fields Inflammation/Immunology
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JZP-MA-11 is a brain-penetrant positron emission tomography (PET) ligand targeting the brain endocannabinoid α/β-hydrolase domain 6 (ABHD6) enzyme. JZP-MA-11 selectively inhibits ABHD6 with an IC50 value of 126 nM. [18F]JZP-MA-11 has the potential for preclinical evaluation targeting the brain ABHD6 in mice and nonhuman primate (NHP) .
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AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications .
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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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Cat. No.: HY-138693
CAS No.: 1186236-75-8
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ST4070 is a potent, orally active, and selective reversible fatty acid amide hydrolase (FAAH) inhibitor. ST4070 increases endocannabinoid (eCB) brain levels and counteracts neuropathic pain in animal models. ST4070 enhances the endogenous eCB tone in specific brain regions engaged in emotional control, and induces remarkable anxiolytic-like behaviours in rodents. ST4070 can be used for neuropathic pain and anxiety disorders research .
Cat. No.: HY-W127407
CAS No.: 201738-25-2
Cat. No.: HY-121517
CAS No.: 86672-58-4
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URB754 is a potent inhibitor of the endocannabinoid-deactivating enzyme monoacylglycerol lipase (MGL) with an IC50 of 200 nM .
Cat. No.: HY-103341
CAS No.: 390824-20-1
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UCM707, a potent and selective inhibitor of endocannabinoid uptake, potentiates hypokinetic and antinociceptive effects of Anandamide .
Cat. No.: HY-103340
CAS No.: 439080-01-0
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O-2093 is a selective endocannabinoid anandamide (AEA) reuptake inhibitor with IC50 of 17.3 μM .
Cat. No.: HY-162305
CAS No.: 2770967-08-1
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MAGL-IN-15 (Compound 6) is a MAGL inhibitor that can be used in the research of diseases and disorders related to the regulation of endocannabinoid system signaling activities .
Cat. No.: HY-120300
CAS No.: 213738-77-3
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UCM710 is an endocannabinoid (eCB) hydrolysis inhibitor that increases the levels of N-arachidonoyl ethanolamine and 2-arachidonoylglycerol in neurons. UCM710 inhibits fatty acid amide hydrolase and α/β-hydrolase domain 6, but not monoacylglycerol lipase .
Cat. No.: HY-103338
CAS No.: 251908-92-6
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AM1172 is metabolically stable anandamide uptake inhibitor. AM1172 inhibits [ 3H] anandamide transport in rat cortical neurons and human CCF-STTG1 astrocytoma cells with IC50 values of 2.1 μM and 2.5 μM, respectively. AM1172 can significantly inhibit AEA hydrolysis and concurrently decrease AEA uptake. AM1172 can be used for the study of endocannabinoid system regulation .
Cat. No.: HY-W777527
CAS No.: 1185244-71-6
Synonyms: NA-Gly-d8
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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
