2-ag

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).

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

TREM2 agonist-2 (I-192) is an orally active and potent agonist of myeloid triggered receptor 2 (TREM2) for neurodegenerative disease research.

CB2 receptor agonist 2 (ZINC72105556) is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor, Ki = 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.

TREM2 agonist-1 (I-246) is a triggering receptor expressed on myeloid cells-2 (TREM2) agonist with an EC50 ranging from 3.0 μM to 100 μM.

rel-5-(4-Chloro-2-fluorophenyl)-2,3-dimethyl-7-[(2R,4S)-tetrahydro-2-(1-methyl-1H-pyrazol-4-yl)-2H-pyran-4-yl]pyrido[3,4-b] The EC50 value of pyrazine against TREM2 was ≤ 0.05 μM and the E.max value was > 250 μM.

Noladin ether (2-AG ether) is a selective and potent cannabinoid CB1 receptor agonist, reducing sensory nerve transmission in rat mesenteric artery beds through a non-CB1/CB2 G(i/o) receptor pathway in a concentration-dependent manner.

LY2979165 (mGlu2 agonist) is an orthosteric agonist of mGluR2 and can be used in studies about serving as an anti-depressant.

NOD2 agonist 1 (compound 3) is a potent NOD2 activator with an EC50 of 4.6 nM.

TRPV1/CB2 agonist 1 (compound 41) is a dual agonist targeting hTRPV1 and CB2 receptors, with an EC50 value of 26.8 μM for hTRPV1. It is applicable in research related to the nervous system.

NOD2agonist 3 (Compound 5) is an effective NOD2 agonist with an EC50 value of 111.45 nM, demonstrating immunoenhancing properties.

NOD2 agonist 2 (compound 23) enhances antigen presentation in murine bone marrow-derived dendritic cells (BMDCs), highlighting its potential as a vaccine adjuvant.

FFA2 agonist-1 (Compound 4) is an agonist of the free fatty acid receptor 2 (FFA2/GPR43) with an EC50 of 81 nM. It demonstrates activity in β-arrestin-2 recruitment and cAMP inhibition assays, with EC50 values of 1.2 μM and 0.53 μM, respectively. FFA2 agonist-1 can induce the mucosal response of appetite-regulating peptide YY (PYY), inhibit fat accumulation, and affect intestinal function and food intake, making it useful for obesity research.

Aβ1–42 aggregation inhibitor 2 (compound 7c) is a potent inhibitor of Aβ1-42 aggregation, playing a significant role in Alzheimer's disease research. It exhibits excellent antioxidant properties, metal ion chelation ability, reduces oxidative stress, and demonstrates neuroprotective and anti-neuroinflammatory activities.

mGluR2 agonist1 hydrochloride is a potent and selective agonist of the metabotropic glutamate receptor (mGluR2), with an EC50 of 82 nM.

mGluR2 agonist1 (Compound 5b) is a potent and selective metabotropic glutamate receptor 2 (mGluR) agonist with an EC50 of 82 nM. It is applicable for research in central nervous system (CNS) disorders.

TREM2 agonist-3 (Compound 4i) is a direct TREM2 agonist (Kd=19.0 µM), and its Kd value for TREM1 is 39.8 µM. It induces Syk phosphorylation and enhances microglial cell phagocytosis, and can be used for the study of neurodegenerative diseases.

TREM2 agonist-4 (Compound 4a) is a TREM2 agonist with a Kd value of 45.9 μM. It activates the TREM2 downstream signaling pathways and enhances the phagocytic function of microglia. TREM2 agonist-4 is applicable for research into neurodegenerative diseases such as Alzheimer's disease.

Aβ1–42 aggregation inhibitor 3 (Compound 3b) is an inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), with IC50 values of 1.634 μM and 0.0285 μM, respectively. It effectively prevents the aggregation of Aβ1-42 and is applicable for Alzheimer's disease (AD) research.

TREM2 agonist-5 is a ligand for the microglial lipid-sensing receptor (TREM2) and acts as an agonist with a Kd of 71.36 μM. It is the racemic analog of the TREM2 agonist VG-3927 and demonstrates excellent microglial phagocytic activity in HEK293-hTREM2/DAP12 cells, effectively activating TREM2 signaling. TREM2 agonist-5 has superior in vitro pharmacokinetics compared to VG-3927 and is potentially useful for Alzheimer's disease research.

CB1/2 agonist 3 is a competitive and potent CB1/CB2 agonist with high affinity for hCB1 and hCB2 and can be used to study neurological disorders.

CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand with Ki values of 3.5 nM and 1.2 nM, respectively. It acts as a full agonist of CB1 and a competitive inverse agonist of CB2. BACE-IN-1 shares these properties, being a complete agonist of CB1 and a competitive inverse agonist of CB2.

CB1/2 agonist 4 (compound 24) is a CB1 full agonist (EC50: 15.09 nM) and a CB2 partial agonist (EC50: 1.16 nM). CB1/2 agonist 4 has significant anti-harm-sensing activity and also activates cannabinoid and TRPV1 receptors (IC50: 0.8 μM, EC50: 0.12 μM). , EC50: 0.12 μM).

CB1/2 agonist 1 is a potent CB1/2 agonist that crosses the blood-brain barrier, acting on CB1R (EC50: 56.15 nM) and CB2R (EC50: 11.63 nM). It reduces glutamate release and LPS-induced microglia activation, exhibiting anti-inflammatory and analgesic activities, with potential for multiple sclerosis studies.