CB1 Selective Inhibitors | 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|
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|
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|
AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
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.
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||human CB1 receptor, Ki: 48.3 nM; rat CB1 receptor, Ki: 55.4 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|
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|
Olivetol (5-Pentylresorcinol, 5-n-Amylresorcinol) is a naturally occurring organic compound being a precursor in various syntheses of tetrahydrocannabinol. It acts as a competitive inhibitor of the cannabinoid receptors CB1 and CB2.
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