Cannabinoid Receptor Inhibitor

Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding K_i of 0.13 nM for the human CB1R in vitro.

AM404, an inhibitor of endocannabinoid reuptake, blocks anandamide transport with IC₅₀ values in the low micromolar range. AM404 is able to relax rat isolated hepatic arteries contracted with Phenylephrine, with a pEC₅₀ value of 7.4 (corresponding to an EC₅₀ of 0.04 μM). Neuroprotective Effect.

Pregnenolone-d₄-1 is the deuterium labeled Pregnenolone. 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-d₄ sodium is the deuterium labeled Pregnenolone monosulfate sodium (HY-110189) . 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-d₄ is the deuterium labeled Pregnenolone. 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.

Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.

Heptadecanoyl ethanolamide is an endogenous cannabinoid. Heptadecanoyl ethanolamide is a synthetic analog of PEA which incorporates an odd-numbered (17-carbon) fatty acid chain.

11(Z),14(Z)-Eicosadienoic acid ethanolamide (Compound 3) is an ethanolamide-conjugated form of 11(Z),14(Z)-Eicosadienoic acid (HY-149589). 11(Z),14(Z)-Eicosadienoic acid ethanolamide inhibits the inactivating transport of an endogenous cannabinoid substance with an IC₅₀ value of 10.6 μM. 11(Z),14(Z)-Eicosadienoic acid ethanolamide can be used for research of neuropsychiatric conditions.

TC-C 14G (Compd 14g) is a Cannabinoid-1 Receptor (CB1R) inverse agonist, with a K_i of 4 nM and EC₅₀ of 11 nM for HCB1R, respectively.

UCM710 is an endocannabinoid (eCB) hydrolysis inhibitor that increases the levels of N-arachidonoyl ethanolamine and 2-arachidonoylglycerol in neurons. UCM710 inhibits fatty acid amide hydrolase and α/β-hydrolase domain 6, but not monoacylglycerol lipase.

N-(3-Hydroxyphenyl)-arachidonoyl amide (Compound 23) is an anandamide transport inhibitor with an IC₅₀ of 21.3 μM.

UCM707, a potent and selective inhibitor of endocannabinoid uptake, potentiates hypokinetic and antinociceptive effects of Anandamide.

O-Arachidonoyl glycidol (compound 1) is a 2-arachidonoylglycerol (2-AG) analog. O-Arachidonoyl glycidol inhibits cytosolic 2-oleoylglycerol (2-OG) hydrolysis with an IC₅₀ value of 4.5 µM. O-Arachidonoyl glycidol blocks 2-OG hydrolysis in membrane fractions and anandamide hydrolysis with IC₅₀s of 19, 12 µM, respectively.

Pregnenolone monosulfate (sodium)-¹³C₂,d₂ is the ¹³C- and deuterium labeled Pregnenolone monosulfate sodium. 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 salt 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 salt can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

SGC stimulator 2 is an orally active soluble guanylyl cyclase (sGC) stimulator with an EC₅₀ of 44 nM. SGC stimulator 2 exhibits inhibitory activity against the CB₂ receptor, with an IC₅₀ of 2.7 μM. SGC stimulator 2 activates native (Fe²⁺) sGC in a heme-dependent manner. SGC stimulator 2 produces sustained hypotensive effects in animal models. SGC stimulator 2 can be used for the research of hypertension.

Yangonin (Standard) is the analytical standard of Yangonin. This product is intended for research and analytical applications. Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.

Palmitoylisopropylamide is a Palmitoylethanolamide analogue inhibits [³H]-Anandamide metabolism with a pI₅₀ of 4.89.

Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively.

Taranabant ((1R,2R)stereoisomer) (Standard) is the analytical standard of Taranabant ((1R,2R)stereoisomer) (HY-10013B). This product is intended for research and analytical applications. Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.

Pregnenolone monosulfate (sodium) (Standard) is the analytical standard of Pregnenolone monosulfate (sodium). This product is intended for research and analytical applications. 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.