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Cannabinoid Receptor

Cannabinoid receptors are of a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid receptors contain seven transmembrane spanning domains. Cannabinoid receptors are activated by three major groups of ligands: endocannabinoids, produced by the mammillary body;[citation needed] plant cannabinoids (such as cannabidiol, produced by the cannabis plant); and synthetic cannabinoids (such as HU-210). All of the endocannabinoids and phytocannabinoids (plant based cannabinoids) are lipophilic, such as fat soluble compounds.

  • CB2 modulator 1
    T10696666261-80-9In house
    CB2 modulator 1 is a potent CB2 modulator. It can be used for the research for immune disorders, osteoporosis, inflammation, renal ischemia.
    • $30
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  • β-Caryophyllene
    T911487-44-5
    β-Caryophyllene ((-)-(E)-Caryophyllene) acts as an CB2 receptor agonist.
    • $41
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  • 2,3-Butanediol
    T19094513-85-9
    2,3-Butanediol is a biotransformed butanediol derived from natural resources.
    • $40
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  • Hemopressin (rat) acetate(568588-77-2 free base)
    TP1901L1
    Hemopressin (rat) 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 CB2 cannabinoid receptors. Hemopressin exerts antinocicep
    • $412
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  • CB2R/FAAH modulator-2
    T677452876918-68-0
    CB2R/FAAH modulator-2 (compound 26) is a dual modulator targeting at CB2R and FAAH. CB2R/FAAH modulator-2 acts as a CB2R agonist and FAAH inhibitor, the Ki values are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 has studies research value related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.
    • $31
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  • Pregnenolone acetate
    TC00191778-02-5
    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
    • $50
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  • GW 833972A
    T643941092502-33-4In house
    GW 833972A is a selective CB2 receptor agonist.GW 833972A has an inhibitory effect on induced neural depolarization and on citric acid-induced cough in an animal model.
    • $350
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  • OMDM-5
    T12306616884-66-3
    OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).
    • $148
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  • CB2R/FAAH modulator-1
    T67896928892-60-8
    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.
    • $117
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  • RVD-Hpα acetate(1193362-76-3 free base)
    TP1939L1
    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
    • $225
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  • OMDM-6
    T12307616884-67-4In house
    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.
    • $195
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  • CB1 inverse agonist 1
    T10694852315-00-5In house
    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.
    • $117
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  • JHU 75528
    T77634947696-17-5In house
    JHU 75528 (JHU-75528) is a novel PET tracer with inhibitory effects on CB that can be used to study the cannabinoid system in schizophrenic patients.
    • $195
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  • Hemopressin (human, mouse) acetate
    TP1900L1
    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
    • $255
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  • Drinabant
    T21861358970-97-5In house
    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.
    • $79
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  • AM-1235
    T29930335161-27-8In house
    AM-1235 is a potent and selective cannabinoid receptor CB1 agonist.
    • $350
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  • NESS 0327
    T22114494844-07-4In house
    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.
    • $127
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  • CB2 receptor agonist 2
    T220091314230-75-5In house
    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.
    • $118
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  • PSNCBAM-1
    T28468877202-74-9In house
    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.
    • $48
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  • GP 1a
    T41231511532-96-0In house
    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.
    • $51
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  • CB 65
    T41230913534-05-1In house
    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.
    • $66
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  • JD-5037
    T44531392116-14-1
    JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.
    • $37
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  • WIN 55,212-2 Mesylate
    T4458131543-23-2
    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.
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    • Rimonabant
      T1519L168273-06-1
      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.
      • $42
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    • AM251
      T1915183232-66-8
      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).
      • $43
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    • (R)-Monlunabant
      T835332765579-76-6
      (R)-Monlunabant ((R)-MRI-1891) serves as a CB1 receptor antagonist utilized in obesity and metabolic disease research [1].
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    • PSB-SB-487
      T89751399049-81-0
      PSB-SB-487 is antagonist of GPR55.
      • $54
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    • Monlunabant
      T791372712480-46-9
      Monlunabant ((S)-MRI-1891), a solid dispersion compound, functions as an inhibitor of the cannabinoid CB1 receptor [1].
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    • CB2R agonist 2
      T82770
      CB2R agonist 2 (cis-17-para) is a CB2R agonist [1].
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    • CB2R agonist 3
      T82769
      CB2R agonist 3, a potent activator of cannabinoid receptor 2 (CB2R), exhibits an EC50 value of 0.37μM, indicative of its significant role in the immune system [1].
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    • Evofolin B
      TN24081961305-60-1
      Evofolin B is a natural compound isolated from the stem bark of Zanthoxylum ailanthoides. Evofolin B has an inhibitory effect on the superoxide anion produced by human neutrophils in response to formyl-L-methionine-L-leucine-L-phenylalanine/cytochalasin B (fMLP/CB).
      • $3,560
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    • CB2R/FAAH modulator-3
      T677472876918-67-9
      CB2R/FAAH modulator-3 (compound 27) is a modulator targeting at CB2R and FAAH. CB2R/FAAH modulator-3 acts as a CB2R agonist and FAAH inhibitor, the Ki values are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 has research value related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.
      • $38
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    • AEF0117
      T799091610878-71-1
      AEF0117, a signaling-specific inhibitor of cannabinoid receptor 1 (CB1-SSi), inhibits cannabinoid self-administration and behavioral disorders associated with THC, and can be used to study cannabis withdrawal.
      • $30
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    • EHP-101
      T132891818428-24-8
      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.
      • $109
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    • CB1 antagonist 2
      T14881614726-85-1
      CB1 antagonist 2 (AM4113) is caimabinoid 1 (CB1) antagonist which inhibits CB1 in vivo with an IC50 of 25.5 nM.
      • $30
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    • 6-Bromopravadoline
      T41350166599-63-9
      6-Bromopravadoline (WIN 54461) (WIN 54461) is an antagonist of CB1. 6-Bromopravadoline acts as an inhibitor of the binding of [3H]Win 55212-2 (IC 50 =515 nM) reflective of cannabinoid receptor binding [1] [2].
      • $57
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    • MJ 15
      T22984944154-76-1
      MJ 15 is a CB1 receptor antagonist with specificity for the study of obesity-induced diseases.
      • $108
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    • Rimonabant hydrochloride
      T1519158681-13-1
      Rimonabant hydrochloride (SR 141716A) is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.
      • $38
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    • GW 405833
      T7705180002-83-9
      GW 405833 (L-768242) is an agonist of cannabinoid-2 (CB(2)) receptor-selective
      • $34
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    • BML-190
      T64172854-32-2
      BML-190 (Indomethacin morpholinylamide) is a specific CB2 receptor inverse agonist (Ki: 435 nM), with 50-fold selectivity over CB1 receptor.
      • $39
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    • A-836339
      T7375959746-77-1
      A-836339 acts as a potent cannabinoid receptor full agonist which has a higher affinity for the peripheral CB2 receptor (Ki = 0.64 nM) over the central CB1 receptor (Ki = 270 nM). It displays analgesic, anti-inflammatory, and anti-hyperalgesic effects in
      • $39
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    • Taranabant racemate
      T13081701977-00-6
      Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor.
      • $46
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    • Olivetol
      T3736500-66-3
      Olivetol (5-n-Amylresorcinol) (5-pentylresorcinol, 5-pentyl-1,3-benzenediol) is an organic compound found in certain species of lichen; it is also a precursor in various syntheses of tetrahydrocannabinol. Olivetol has an antioxidant effect.
      • $49
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    • CB1R antagonist 1
      T61989334668-69-8
      CB1R antagonist 1 is a potent CB1R antagonist that can be used to study diseases related to the nervous system.
      • $68
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    • O-1602
      T23097317321-41-8
      O-1602 is a novel GPR55 agonist, an atypical cannabinoid associated with the central nervous system and obesity, and is a candidate compound for the treatment of cystitis.O-1602 promotes hepatic steatosis through GPR55 and PI3 kinase / Akt / SREBP-1c signalling in mice.O-1602 induces, in a GPR3-independent manner, in Hep55B cells with elevated intracellular calcium.
      • $41
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    • Tedalinab
      T17027916591-01-0
      Tedalinab is an effective and selective cannabinoid receptor 2 agonist. Tedalinab has the potential for neuropathic pain and osteoarthritis treatment. Tedalinab has >4700-fold functional selectivity for CB2 over CB1.
      • $1,140
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    • Hemopressin(human, mouse) TFA
      T757991431329-48-4
      Hemopressin TFA, a nonapeptide originating from the α1-chain of hemoglobin and initially isolated from rat brain homogenates, is an orally active, selective inverse agonist of CB1 cannabinoid receptors that demonstrates antinociceptive effects in inflammatory pain models [1] [2].
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    • ML-193
      T22103713121-80-3
      ML-193 (CID 1261822) is a potent and selective GPR55 antagonist( IC50 : 221 nM). It shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2, and can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats.
      • $39
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    • (±)-Cannabichromene
      TN357520675-51-8
      (±)-Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1), it selectively reduces inflammation-induced hypermotility in vivo in a manner that is not dependent on cannabinoid receptors or TRPA1.
      • $173
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    • Tetrahydromagnolol
      TN226820601-85-8
      Tetrahydromagnolol can activate cannabinoid (CB) receptors.
      • $50
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