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	hCB1, Ki: 0.7 nM; rCB1, Ki: 2.8 nM
S6735	JD-5037	JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor.	Selective	CB1 receptor, IC50: 2 nM
S3021	Rimonabant (SR141716)	Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3.	Selective	hCB1, IC50: 13.6 nM
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
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
S0412	Bay 59-3074	Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. Bay 59-3074 displays analgesic properties.	Pan	rat CB1 receptor, Ki: 55.4 nM; human CB1 receptor, Ki: 48.3 nM
S8017	WIN 55, 212-2 mesylate	WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission.	Pan	CB1, Ki: 62.3 nM
S1544	AM1241	AM-1241 is a selective cannabinoid CB2 receptor agonist with K_i of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.	Pan	CB1, Ki: 280 nM