MAGL

MAGL-IN-5 is a non-selective lipase inhibitor.

MAGL-IN-1 is a selective and potent monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 80 nM.

MAGL-IN-4 (His121 ARG57) is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.

JJKK 048 is a potent and selective MAGL inhibitor.

JZP-430 is an effective, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) (IC50: 44 nM). It also shows ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).

JNJ-42226314 is a highly selective non-covalent monoacylglycerol lipase (MAGL) inhibitor with anti-injury effects.JNJ-42226314 shows efficacy via endogenous cannabinoid-2-acryloylglycerol (2-AG) in models of neuropathic pain and inflammatory pain.

SA57 is a potent, selective inhibitor of FAAH(IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH).

JW 642 is an effective inhibitor of monoacylglycerol lipase (MAGL) (IC50: 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively).

PF-06795071 is an effective and selective covalent inhibitor of MAGL (IC50: 3 nM).

WWL70 is a selective inhibitor of alpha/beta hydrolase domain 6 with an IC50 of 70 nM.

JZL195 is a selective and efficacious dual FAAH/MAGL inhibitor.

JZP-361 is a specific MAGL inhibitor with IC50s of 46 nM, 7.24 μM, and 1.79 μM for human recombinant MAGL, human recombinant FAAH, and human hABHD6. JZP-361 displays anti-histaminergic activities. JZP-361 can be used in studies about asthma.

NF-1819 is a potent and selective irreversible MGL (β-lactam-based monoacylglycerol lipase) inhibitor. NF-1819 alleviates symptoms in a MS model in vivo and exhibits analgesic effects in an acute inflammatory pain model in vivo. NF-1819 displays high membrane permeability and brain penetrant.

KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human/mouse/rat MAGL (IC50: 5.9/15/43 nM). It has not inhibitory for FAAH (IC50 > 50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).

ABX-1431 (Elcubragistat) is a selective and orally available CNS-penetrant monoacylglycerol lipase (MAGL/MGLL) inhibitor (IC50: 14 nM).

Euphol, an alcohol tetracyclic triterpene, has a wide range of pharmacological properties and is considered to have anti-inflammatory action.

MJN110 (Cravatt Reagent) is a potent and selective MAGL inhibitor. Cravatt Reagent inhibits MAGL (IC50 = 9.1 nM). MJN110(Cravatt Reagent) Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model.

JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.

AM6701 is an effective dual inhibitor of FAAH (fatty acid amide hydrolase) and MAGL (monoacylglycerol lipase), with an IC50 of 1.2 nM. It exhibits neuroprotective effects by modulating endogenous cannabinoids and inhibiting calpain-mediated excitotoxic brain injury.

ML226 is a α/β hydrolase domain-containing protein 11 (ABHD11) inhibitor that inhibits ABHD11 in vitro and in situ.

AA38-3 (1-Piperidinecarboxylic acid, 4-nitrophenyl ester) inhibites three SHs (ABHD6, ABHD11, and FAAH)

MAGL-IN-21 (Compound (S)-6) is a selective inhibitor of monoacylglycerol lipase (MAGL) with an IC50 of 1.59 nM.

MAGL-IN-22 (Compound 40) is a reversible, competitive, and selective inhibitor of MAGL that is capable of crossing the blood-brain barrier, with an IC50 of 0.34 μM for hMAGL. It exhibits significant antioxidant and anti-inflammatory properties, activating the Nrf2 pathway and markedly suppressing NFκB-mediated inflammation, without inducing cytotoxic effects. MAGL-IN-22 is applicable in research on neurodegenerative diseases, chronic pain, and cancer.

FAAH/MAGL-IN-1, also known as compound SIH 3, is a highly effective inhibitor of FAAH (fatty acid amide hydrolase) and MAGL (monoacylglycerol lipase). It exhibits IC50 values of 31 nM and 29 nM against FAAH and MAGL, respectively. This compound shows promising potential for advancing research in the field of neuropathic pain [1].