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Cannabinoid Receptor Type 1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Cannabinoid Receptor (16) 5-HT Receptor (1) Androgen Receptor (1) Endogenous Metabolite (2) Fatty Acid Synthase (FASN) (1) Isotope-Labeled Compounds (2) NO Synthase (1) PERK (1) TRP Channel (2)
By Research Areas:	Cancer (1) Endocrinology (1) Inflammation/Immunology (2) Metabolic Disease (4) Neurological Disease (14)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Cannabinoid Receptor C-type Lectin-like Receptors (CTLRs) PCSK9 Scavenger Receptor Class B type I (SR-BI）

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-110028

Leelamine hydrochloride	Cannabinoid Receptor Fatty Acid Synthase (FASN) Androgen Receptor	Endocrinology Cancer
Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees . Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis ^[2,3].

HY-116649

CB1 antagonist 2 AM4113	Cannabinoid Receptor	Neurological Disease Metabolic Disease
CB1 antagonist 2 (AM4113) is an orally active cannabinoid receptor type 1 (CB1R) antagonist. CB1 antagonist 2 suppresses appetite, reduces body weight, and blocks addictive behaviors such as heroin addiction, without causing adverse effects like nausea and depression that are associated with traditional CB1 inverse agonists. CB1 antagonist 2 can be used in studies related to obesity and opioid addiction .

HY-113421

Linoleoyl ethanolamide Linoleic acid monoethanolamide	Cannabinoid Receptor	Neurological Disease
Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2 receptors, and inhibits the binding of ^[3H]CP-55,940 with K_is of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .

HY-113421S

Linoleoyl ethanolamide-d4	Isotope-Labeled Compounds Cannabinoid Receptor	Neurological Disease
Linoleoyl ethanolamide-d4 is a deuterated labeled Linoleoyl ethanolamide . Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2 receptors, and inhibits the binding of ^[3H]CP-55,940 with K_is of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .

HY-172587

CB1R Allosteric modulator 5	Cannabinoid Receptor	Neurological Disease
CB1R Allosteric modulator 5 (compound 3) is a selective, and blood-brain barrier (BBB) permeable **Cannabinoid receptor type 1** allosteric modulator with a pIC₅₀ of 6.89. CB1R Allosteric modulator 5 attenuates both cocaine-seeking behavior specific to cue-induced reinstatement and cocaine-induced behavioral sensitization without altering locomotor activity .

HY-N6097

Amauromine	Cannabinoid Receptor	Neurological Disease
Amauromine is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist with K_i and K_b values of 178 nM and 66.6 nM, respectively .

HY-141411

(Rac)-Zevaquenabant (Rac)-MRI-1867	Cannabinoid Receptor NO Synthase	Others
(Rac)-Zevaquenabant ((Rac)-MRI-1867, compound 6b) is a cannabinoid receptor type 1 (CB₁R)/iNOS antagonist, with a K_i of 5.7 nM for CB₁R. (Rac)-Zevaquenabant is potential for the research of liver fibrosis .

HY-145196

RTICBM-189	Cannabinoid Receptor	Neurological Disease
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB₁) receptor with a pIC₅₀ of 7.54 in Ca ²⁺ mobilization assay. RTICBM-189 has pIC₅₀s of 5.29 and 6.25 for hCB₁ and mCB₁, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats .

HY-144827

AM8936	Cannabinoid Receptor	Neurological Disease Metabolic Disease
AM8936 acts as a balanced and potent cannabinoid receptor type-1 (CB1) agonist in functional assays (EC₅₀s of 8.6 and 1.4 nM for rCB1 and hCB1, respectively). AM8936 exhibits high affinity for rat CB1 (rCB1) with K_i of 0.55 nM. AM8936 is a potent and efficacious CB1 agonist in vivo. AM8936 can be used for the research of CNS and metabolic disorders, pain, glaucoma, etc .

HY-107019

Surinabant SR 147778	Cannabinoid Receptor	Metabolic Disease
Surinabant (SR 147778) is an orally active, selective cannabinoid receptor type 1 CB1R antagonist. Surinabant is used in studies of obesity and alcoholism .

HY-135882

OMDM-6	TRP Channel Cannabinoid Receptor Endogenous Metabolite	Neurological Disease
OMDM-6 is a hybrid agonist of *vanilloid receptor* type 1 (VR1, TRPV1) (EC₅₀*=75 nM) and cannabinoid* receptor type 1 (CB1) (K_i=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a K_i of 7.0 μM .

HY-135881

OMDM-5	TRP Channel Endogenous Metabolite	Neurological Disease
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a K_i of 4.8 μM. OMDM-5 is also a potent *vanilloid receptor* type 1 (VR1, TRPV1) agonist, with an EC₅₀** of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (K_i=4.9 μM) .

HY-112707

AM9405	Cannabinoid Receptor 5-HT Receptor	Neurological Disease
AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. AM9405 inhibits twitch contraction of the ileum and the colon with IC₅₀s of 45.71 and 0.076 nM, respectively.

HY-174838

CB1-IN-3	Cannabinoid Receptor	Neurological Disease Metabolic Disease Inflammation/Immunology
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 .

HY-W770198

2-Linoleoyl glycerol-d5 2-Monolinolein-d₅; 2-Monolinoleoylglycerol-d₅	Isotope-Labeled Compounds Cannabinoid Receptor	Neurological Disease
2-Linoleoyl glycerol-d₅ (2-Monolinolein-d₅; 2-Monolinoleoylglycerol-d₅) is the deuterium labeled 2-Linoleoyl glycerol (HY-130311). 2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .

HY-153693

CB2 receptor agonist 4	Cannabinoid Receptor	Neurological Disease Inflammation/Immunology
CB2 receptor agonist 4 (Compound 8) is a highly selective cannabinoid receptor type 2 (CB2 Receptor) agonist with an EC₅₀ of 13.99 nM. CB2 receptor agonist 4 shows no significant activity against cannabinoid receptor type 1. CB2 receptor agonist 4 can be used for the research of pain and immune-related diseases .

HY-120093

GAT100	Cannabinoid Receptor PERK	Neurological Disease
GAT100 is a negative allosteric modulator and covalent allosteric probe for cannabinoid receptor type 1 (CB1R). GAT100 acts as a positive allosteric modulator for orthosteric agonist CP55,940 binding to regulate the CB1R signaling pathway. GAT100 reduces the potency and efficacy of orthosteric CB1R agonists in terms of β-arrestin 1 recruitment, phosphorylation of PLCβ3 and ERK1/2, cAMP accumulation, and CB1R internalization. GAT100 is applicable to the research of psychobehavioral and somatic diseases .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-110028

Leelamine hydrochloride	other families Classification of Application Fields Pinaceae Terpenoids Diterpenoids Plants Disease Research Fields Pinus massoniana Lamb. Endocrinology Source Classification	Cannabinoid Receptor Fatty Acid Synthase (FASN) Androgen Receptor
Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees . Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis ^[2,3].

HY-113421

Linoleoyl ethanolamide Linoleic acid monoethanolamide	Human Gut Microbiota Metabolites Microorganisms Endogenous metabolite Source Classification	Cannabinoid Receptor
Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2 receptors, and inhibits the binding of ^[3H]CP-55,940 with K_is of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .

HY-N6097

Amauromine	Alkaloids Microorganisms Indole Alkaloids Source Classification	Cannabinoid Receptor
Amauromine is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist with K_i and K_b values of 178 nM and 66.6 nM, respectively .

HY-135882

OMDM-6	Alkaloids Monophenols Neurological Disease Classification of Application Fields Other Alkaloids Phenols Endogenous metabolite Disease Research Fields Source Classification	TRP Channel Cannabinoid Receptor Endogenous Metabolite
OMDM-6 is a hybrid agonist of *vanilloid receptor* type 1 (VR1, TRPV1) (EC₅₀*=75 nM) and cannabinoid* receptor type 1 (CB1) (K_i=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a K_i of 7.0 μM .

HY-135881

OMDM-5	Alkaloids Monophenols Neurological Disease Classification of Application Fields Other Alkaloids Phenols Endogenous metabolite Disease Research Fields Source Classification	TRP Channel Endogenous Metabolite
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a K_i of 4.8 μM. OMDM-5 is also a potent *vanilloid receptor* type 1 (VR1, TRPV1) agonist, with an EC₅₀** of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (K_i=4.9 μM) .

Cat. No.	Product Name	Chemical Structure

HY-113421S

Linoleoyl ethanolamide-d4
Linoleoyl ethanolamide-d4 is a deuterated labeled Linoleoyl ethanolamide . Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2 receptors, and inhibits the binding of ^[3H]CP-55,940 with K_is of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .

Linoleoyl ethanolamide-d4

Linoleoyl ethanolamide-d4 is a deuterated labeled Linoleoyl ethanolamide . Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2 receptors, and inhibits the binding of ^[3H]CP-55,940 with K_is of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .

HY-W770198

2-Linoleoyl glycerol-d5
2-Linoleoyl glycerol-d₅ (2-Monolinolein-d₅; 2-Monolinoleoylglycerol-d₅) is the deuterium labeled 2-Linoleoyl glycerol (HY-130311). 2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .

2-Linoleoyl glycerol-d5

2-Linoleoyl glycerol-d₅ (2-Monolinolein-d₅; 2-Monolinoleoylglycerol-d₅) is the deuterium labeled 2-Linoleoyl glycerol (HY-130311). 2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .

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