cb 2

CB2 modulator 1 is a potent CB2 modulator. It can be used for the research for immune disorders, osteoporosis, inflammation, renal ischemia.

CB2R-IN-1 is a potent inverse agonist of the cannabinoid CB2 receptor (Ki: 0.9 nM).

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.

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.

GP 2A is a selective agonist of CB2 receptor.

CB2 receptor agonist 9 (Compound 33) is an orally active agonist of cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. It inhibits the expression of TNF-α, IL-1β, and IL-6, demonstrating anti-inflammatory activity in a DSS-induced acute colitis model in mice.

CB2 receptor agonist 8 (Compound 17) is an agonist of the cannabinoid receptor 2 (CB2 receptor). It shows cytotoxicity in U87, RPMI 8226, HL-60, and L929 cells with IC50 values of 91.03, 16.29, 23.51, and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expression of pro-apoptotic genes BAX, BAD, BIM, and the tumor suppressor gene p53, and induces apoptosis in U87 cells. Additionally, it inhibits the migration of U87 cells.

CB2receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor CB2R, with a binding affinity (Kd) of 39 nM. This compound serves as a tool for synthesizing various CB2R probes.

CB2 receptor antagonist 4 is a selective inverse agonist for the CB2 receptor with a Kd value of 39 nM.

CB2receptor agonist 6 (compound 70) is a CB2R agonist with an EC50 of 162 nM. It has IC50 values of 4.83 μM for CB1R and 0.88 μM for CB2R. As a neuroprotective agent, CB2receptor agonist 6 is useful for research in neurological disorders.

Hexyl resorcinol derivative 29 is a CB2 selective competitive antagonist/reverse agonist demonstrating notable potency. Meanwhile, Olivanol and 5-(2-methyloctane-2-yl) resorcinol derivatives 23 and 24 exhibit substantial antinociceptive effects. Notably, compound 24 activates both cannabinoid and TRPV1 receptors.

CB2 PET Radioligand 1 (compound [18F]9) is a positron emission tomography (PET) radioligand with high affinity for the human cannabinoid receptor 2 (hCB2, Ki=7.7 nM). It is synthesized via Cu-mediated 18F-fluorination and demonstrates significant brain uptake in a mouse model of neuroinflammation [1].

Compound 39, also known as CB2 receptor antagonist 2, is a potent CB2 antagonist exhibiting an IC50 of 0.33 μM. It engages in strong interactions with residues L17, W6.48, V6.51, and C7.42 [1].

CB1 inverse agonist 1 (MRL-650) is an orally active and selective CB1 agonist. The IC50s for CB1 and CB2 are 7.5 nM and 4100 nM, respectively. CB1 inverse agonist 1 shows anorexigenic effects.

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

β-Caryophyllene ((-)-(E)-Caryophyllene) acts as an CB2 receptor agonist.

EHP-101 (VCE-004.8) is a specific dual agonist of PPARγ and CB2 receptor with potent anti-inflammatory activity. EHP-101 attenuates adipogenesis and prevents diet-induced obesity.

Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM). In rat models of chronic neuropathic and inflammatory pain, it displays anti-hyperalgesic and antiallodynic properties.

GW 405833 (L-768242) is an agonist of cannabinoid-2 (CB(2)) receptor-selective

OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor with a Ki of 2.4 μM.

OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).

Anandamide ((5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide), an immune modulator, acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55) in the central nervous system.

BAY 38-7271 has strong neuroprotective properties.[1] BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist. With Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively.

SR144528 is an antagonist of the CB2 receptor (Ki = 0.6 nM) and inhibits microsomal ACAT activity (IC50 = 3.6 μM).