CB1 Selective Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
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.

Selective rCB1, Ki: 2.8 nM; hCB1, Ki: 0.7 nM
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.

Selective hCB1, IC50: 13.6 nM
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.

Selective
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.

Selective
S1544 AM1241

AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.

Pan CB1, Ki: 280 nM