CB1 Inhibitor

Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

2-Linoleoyl glycerol (2-Monolinolein) is a partial CB1 receptor agonist with a pEC₅₀ of 4.781. 2-Linoleoyl glycerol activates the hCB1 receptor. 2-Linoleoyl glycerol does not induce an increase in intracellular free Ca²⁺. 2-Linoleoyl glycerol can be used in the research of neurological disorders.

Pregnenolone (Standard) is the analytical standard of Pregnenolone. This product is intended for research and analytical applications. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC₅₀ and a K_i of 1.79 μM and 0.72 μM, respectively.

Auriculasin is an anticancer agent that inhibits VEGFR2, PI3K/AKT/mTOR, MAPK. Auriculasin can inhibit cell proliferation, induce cell apoptosis, and inhibit angiogenesis, and promotes mitochondrial oxidative stress and ferroptosis. Auriculasin is also active at the cannabinoid receptor CB1 with an IC₅₀ of 8.92 μM. Auriculasin can be used in cancer research, especially related diseases such as prostate cancer and non-small cell lung cancer, as well as research on the development of anti-angiogenic drugs.

JTE-907 is a selective and orally active cannabinoid CB2 receptor inverse agonist and exerts anti-inflammatory effects. JTE-907 upregulates IL-6, MCP-1, IL-1β, VEGF, ANGPTL4, and TRPV1 in mature adipocytes. JTE-907 downregulates CB1, MCP-1, and IL-1β in preadipocytes. JTE-907 inhibits ear swelling in mice. JTE-907 reverses the protective effects of CB2 agonists and Anandamide (HY-10863) against cytokine-evoked colonic mucosal damage. JTE-907 can be used for the research of allergic dermatitis, obesity, and colitis.

ANEB-001 is an orally active CB1 inhibitor, can be used to research acute cannabinoid intoxication.

Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoid receptor (CB1) and inhibits FAAH with similar potencies (IC₅₀ = 2 nM).

CB1-IN-2 (Compound 4g) is a selective CB₁ inhibitor with an IC₅₀ of 0.644 μM. CB1-IN-2 can penetrates BBB and might cause CNS side effect similar with Rimonabant.

CB1-IN-3 (Compound 6i) is a potent cannabinoid type 1 receptor (CB1) inhibitor. CB1-IN-3 is promising for research of obesity, inflammation, and neurological diseases.

RTI-371 is a highly selective atypical dopamine transporter (DAT) inhibitor that crosses the blood-brain barrier. RTI-371 exhibits potent inhibitory activity in cell lines transfected with human DAT (IC₅₀ = 8.7 nM) and shows high binding affinity for rat DAT with a K_i value of 7.81 nM. RTI-371 also acts as a positive allosteric modulator of the human cannabinoid 1 receptor (hCB1 receptor), enhancing the activity of cannabinoid receptor agonists in a concentration-dependent manner. RTI-371 can be used for the research of Parkinson's disease.

MRL-650 (CB1 inverse agonist 1), a chemical probe, is a highly potent, orally active, and specific inverse agonist of CB1 receptor with IC₅₀s of 7.5 nM and 4100 nM for CB1 and CB2 receptors, respectively. Anorexigenic effects.