cb1

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.

CB1-IN-1 (DBPR211) is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively.

CB1 agonist 1 is a potent CB1 agonist with a pIC50 value of 5.7 for CB1 receptors.CB1 agonist 1 can be used to study brain disorders, pain, and inflammation.

CB1 antagonist 1 is a CB1 receptor antagonist, used in the research of obesity and metabolic syndrome, neuroinflammatory disorders, cognitive disorders, and gastrointestinal disorders, psychosis, and cardiovascular.

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). CB1/2 agonist 1 reduces glutamate release and LPS-induced microglia activation, and has anti-inflammatory and analgesic activities. CB1/2 agonist 1 has potential for multiple sclerosis studies.

CB1 antagonist 2 (AM4113) is caimabinoid 1 (CB1) antagonist which inhibits CB1 in vivo with an IC50 of 25.5 nM.

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-IN-2 (Compound 4g) is a potent and selective inhibitor of the CB1 receptor, exhibiting an IC50 value of 0.644 μM. This compound possesses the ability to penetrate the blood-brain barrier and has the potential to induce central nervous system (CNS) side effects similar to Rimonabant [1].

CB1 Inverse Agonist 2, an orally active compound, serves as an inverse agonist for the Cannabinoid Receptor CB1. It effectively counteracts the hypothermia and anorexia induced by CP55940 in mouse models.

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

CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a competitive agonist for the CB1/CB2 receptors. It exhibits CB1/CB2 agonistic activity by binding to the human CB1 and CB2 receptors, with Ki values of 5.9 nM and 3.5 nM, respectively [1].

Cannabigerol is a high affinity α±2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist ; also binds to the CB2 receptor; it can relieve interocular pressure, which may be of benefit in the treatment of glaucoma.

ABCB1-IN-1 (compound 3) is a potent inhibitor of ABCB1 that promotes cell apoptosis. Featuring 1-benzylimidazole, it exhibits IC50 values of 1.26 μM for Colo205 cells and 2.21 μM for Colo320 cells, respectively [1].

RCB16007 is a Yellow Fever Virus (YFV) inhibitor that also demonstrates inhibitory action against the West Nile virus with an effective concentration (EC50) of 7.9 μM and a cytotoxic concentration (CC50) of 17 μM [1].

Pregnenolone acetate is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. It acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. It can protect the brain from cannabis intoxication

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

Hemopressin (human, mouse) acetate is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts an

CB2R/FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM.

RVD-Hpα acetate is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. Also high affinity CB2 positive allosteric modulator (Ki

Drinabant (AVE-1625) is an orally active CB1 receptor antagonist. Drinabant inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.

PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo. PSNCBAM-1 can be used for obesity studies.

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.

CB 65 is a high affinity and selective CB2 receptor agonist with Ki values of 3.3 and > 1000 nM for CB2 and CB1 receptors respectively.

NESS 0327 is a high selectivity antagonist of the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor.

AM-1235 is a potent and selective cannabinoid receptor CB1 agonist.

CB1R antagonist 1 is a potent CB1R antagonist that can be used to study diseases related to the nervous system.

INCB13739 is an orally active, potent, selective, and tissue-specific inhibitor of 11β-HSD1 (11β-hydroxysteroid dehydrogenase 1), demonstrating IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC). It is utilized in research for type 2 diabetes mellitus (T2DM) and obesity [1].

CB10-277 is a synthetic derivative of dimethylphenyl-triazene related to dacarbazine, with antineoplastic properties. Related to the agent dacarbazine, CB10-277 is converted in vivo to a monomethyl triazene form that alkylates DNA, resulting in inhibition of DNA replication and repair; in addition, this agent may act as a purine analogue, resulting in inhibition of DNA synthesis, and may interact with protein sulfhydryl groups.

CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arrestin-2 recruitment [1].

CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 with anti-tumor effects. It inhibits MCF-7 cell growth (IC50: 0.82 nM).

Compound 38-S is an orally active CB1R/AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R. This compound activates AMPK and has been shown to decrease food intake and body weight, in addition to enhancing glucose tolerance and insulin sensitivity [1].

CB1R Allosteric modulator 1 (compound 11) is a potent allosteric modulator of CB1R. CB1R Allosteric modulator 1 negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.

KH-CB19 is an effective and highly specific inhibitor of the CDC2-like kinase isoforms 1 and 4 (CLK1/CLK4).

INCB16562 is a novel, selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3. Treatment of myeloma cells with INCB16562 potently inhibited interleukin-6 (IL-6)-induced phosphorylation of STAT3. INCB16562 abrogated the protective effects of recombinant cytokines or bone marrow stromal cells and sensitized myeloma cells to cell death by exposure to dexamethasone, melphalan, or bortezomib. Oral administration of INCB16562 antagonized the growth of myeloma xenografts in mice and enhanced the antitumor activity of relevant agents in combination studies. INCB16562 is a potent JAK1/2 inhibitor and that mitigation of JAK/STAT signaling by targeting JAK1 and JAK2 will be beneficial in the treatment of myeloma patients, particularly in combination with other agents. ( source: Neoplasia. 2010 Jan;12(1):28-38. ).

CB1R Allosteric modulator 3 is a potent CB1R modulator.CB1R Allosteric modulator 3 inhibits cAMP and β-Arrestin, and can be used for the study of obesity and nicotine addiction.

CB1R Allosteric modulator 2 (compound 18) is a potent allosteric modulator of the CB1R receptor. It exhibits negative modulation of the functional activity of orthosteric ligands (NAM) at CB1Rs, as demonstrated in previous studies [1].

TM38837 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.

JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.

6-Iodopravadoline (AM630) is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors.

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.

AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49 nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM).

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.

Otenabant (CP-945598) has been investigated for the treatment of Obesity.

GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.

WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively. Cannabinoid analogue WIN 55,212-2 Mesylate exhibited a novel anticancer effect against human tumors.

AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.

N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. Also high affinity CB2 positive allosteric modulator (Ki = 50 nM).

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.

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

Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a potent nootropic steroid that positively regulates NMDA recordings, and can be used in studies of neuroticism and depression.