Cannabinoid Receptors

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  1. CB2 receptor agonist

    GW842166X is a selective non-cannabinoid CB2 receptor agonist, which is undergoing clinical development as a novel oral treatment for inflammatory pain
  2. CB1 modulator?€?

    Org 27569 is a potent CB1 receptor allosteric modulator (pEC50 = 8.24).
  3. Rimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane.
  4. CB1 receptor inverse agonist

    Rimonabant hydrochloride is a CB1 receptor inverse agonist.
  5. CB1 receptor inverse agonist

    Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
  6. CB2 agonist

    JWH-133 is a potent selective CB2 receptor agonist, with a Ki of 3.4nM and selectivity of around 200x for CB2 over CB1 receptors.
  7. CB receptor agonist

    WIN 55,212-2 is a potent cannabinoid receptor agonist that has been found to be a potent analgesic in a rat model of neuropathic pain. It activates p42 and p44 MAP kinase via receptor-mediated signaling.
  8. CB2 receptor ligand

    BML-190 is a selective inverse agonist of the human cannabinoid CB2 receptor.
  9. CB2 agonist

    MDA 19 is a potent and selective agonist for the cannabinoid receptor CB2, with reasonable selectivity over the psychoactive CB1 receptor.
  10. CB1 antagonist

    CP 945598 is a potent and highly selective CB1 antagonist.
  11. cannabinoid CB2 receptor inverse agonist

    CB2R-IN-1 is a potent cannabinoid CB2 receptor inverse agonist with a Ki of 0.9 nM.
  12. CB2 inverse agonist

    SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.
  13. CB1 receptor antagonist

    AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors.
  14. JWH 250 is a cannabimimetic indole that shows a high-affinity for both the central cannabinoid (CB1) and the peripheral cannabinoid (CB2) receptors
  15. JWH 370 is a (1-naphthoyl)pyrrole analog of JWH 018 that potently activates both CB1 and CB2 receptors (Ki values of 5.6 and 4.0 nM, respectively)
  16. JWH 249 is a synthetic cannabinoid (CB) that potently activates the central CB1 and peripheral CB2 receptors (Ki = 8.4 and 20 nM, respectively).
  17. cannabinoid agonist

    JWH 307 is a (1-naphthoyl)pyrrole cannabimimetic that potently activates both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors (Ki values of 7.7 and 3.3 nM, respectively).
  18. AM1220 is a potent synthetic cannabinoid (CB) with preference for the central CB1 receptor (Ki = 3.88 nM) over the CB2 receptor (Ki = 73.4 nM).
  19. AM2233 is a full agonist of the central cannabinoid (CB1) receptor (Ki = 2.8 nM).
  20. CB2 receptor agonist

    Tedalinab (GRC-10693) is a drug developed for the treatment of osteoarthritis and neuropathic pain, which acts as a potent and selective cannabinoid CB2 receptor agonist. It has a very high selectivity of 4700x for CB2 over the related CB1 receptor, has good oral bioavailability and has shown promising safety results and effective analgesic and antiinflammatory actions in early clinical trials.
  21. CB2 antagonist

    AM630 is a selectivity CB2 antagonist with Ki of 31.2 nM, > 150 fold selectivity over CB1 receptor.
  22. CB1 receptor antagonist

    Otenabant is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.
  23. CB1/CB2 receptor agonist

    Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively .
  24. CB2 receptor agonist

    AM1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.
  25. PPARγ and CB2 receptor dual agonist

    VCE-004.8, a semi-synthetic multitarget cannabinoquinoid, is a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity.
  26. CB1 antagonist

    CB1 antagonist 2 is caimabinoid 1 (CB1) antagonist extracted from patent WO2016184310A1, compound 3, inhibits CB1 in vivo with an IC50 of 25.5 nM.
  27. CB2 agonist

    Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist, with an EC50 of 6.2 nM for hCB2.
  28. CB1 agonist

    Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status.
  29. CBP inhibitor

    GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.
  30. CB1R antagonist

    JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.
  31. CB-1 receptor antagonist

    (±)-Ibipinabant ((±)-SLV319) is the racemate of SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM.
  32. CB1 antagonist/inverse agonist

    Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1.
  33. CB1 receptor inverse agonist

    Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.
  34. immune modulator

    Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55).
  35. cannabinoid (CB2) agonist

    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
  36. CB1/CB2 agonist

    NMP-7 is a non-selective agonist of the CB1 and CB2 cannabinoid receptors that acts by blocking T-type calcium channels.

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