Cannabinoid Receptor

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Cannabinoid Receptor Agonists | Antagonists (7)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S3021 Rimonabant 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.
S1544 AM1241 AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.
  • Sci China Life Sci, 2014, 57(2):201-8
S2819 AM251 AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
S8012 Otenabant (CP-945598) HCl Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1.
S2778 GW842166X 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.
S2854 BML-190 BML-190 is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor.
  • University of Alberta, 2014, Yahya Muhammad Fiteih
S1534 Org 27569 Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S3021 Rimonabant <1 mg/mL 25 mg/mL 2 mg/mL
S1544 AM1241 <1 mg/mL 101 mg/mL <1 mg/mL
S2819 AM251 <1 mg/mL 40 mg/mL <1 mg/mL
S8012 Otenabant (CP-945598) HCl <1 mg/mL 5 mg/mL <1 mg/mL
S2778 GW842166X <1 mg/mL 20 mg/mL <1 mg/mL
S2854 BML-190 <1 mg/mL 22 mg/mL <1 mg/mL
S1534 Org 27569 <1 mg/mL 82 mg/mL <1 mg/mL
Tags: Cannabinoid Receptor signaling | CB1 receptor signaling | CB2 signaling | Cannabinoid Receptor inhibitor review
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