A novel CB1 selective neutral antagonist with low CNS penetration (Ki = 1.7 and 523 nM for CB1 and CB2

AM6545 – 1 mg

Brand:
Cayman
CAS:
1245626-05-4
Storage:
-20
UN-No:
Non-Hazardous - /

Peripherally-restricted cannabinoid receptor 1 (CB1) selective antagonists have the potential to inhibit food intake while also escaping centrally-mediated neuropsychiatric side effects. AM6545 is a novel CB1 selective neutral antagonist with low CNS penetration, exhibiting Ki values of 1.7 and 523 nM for CB1 and CB2 receptors, respectively.{28438} It reduces food intake and food-reinforced behavior, such as time spent feeding, in a dose-dependent manner, resulting in decreased body weight.{28438,28439} AM6545 produces improvements in glucose homeostasis, fatty liver, and plasma lipid profiles in mice with diet-induced obesity.{28440} It does not affect behavior responses that are associated with activation of CB1 receptors in the brain.{28440}  

 

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Description

A novel CB1 selective neutral antagonist with low CNS penetration (Ki = 1.7 and 523 nM for CB1 and CB2, respectively); reduces food intake, food-reinforced behavior and weight gain; improves metabolic profiles of mice with diet-induced obesity

Formal name: 5-[4-(4-cyano-1-butyn-1-yl)phenyl]-1-(2,4-dichlorophenyl)-N-(1,1-dioxido-4-thiomorpholinyl)-4-methyl-1H-pyrazole-3-carboxamide

Synonyms: 

Molecular weight: 556.5

CAS: 1245626-05-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity||Research Area|Neuroscience|Behavioral Neuroscience|Food Intake||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors

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