1245626-05-4
Chemical Structure
AM6545
- CAS. Nr.: 1245626-05-4
- Formula:C26H23Cl2N5O3S
- Molecular Weight:556.46
IUPAC Name: 5-(4-(4-cyanobut-1-yn-1-yl)phenyl)-1-(2,4-dichlorophenyl)-N-(1,1-dioxidothiomorpholino)-4-methyl-1H-pyrazole-3-carboxamide
InChIKey: XBHQLFVDGLPBCK-UHFFFAOYSA-N
SMILES: CC1=C(C2=CC=C(C#CCCC#N)C=C2)N(C3=C(C=C(Cl)C=C3)Cl)N=C1C(NN4CCS(CC4)(=O)=O)=O
Biological Activity: AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications[1][2][3].
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AM6545 | 99.32% | AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications. | ||||||||||||||||||||
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AM6545 (Standard) | ≥98% | AM6545 (Standard) is the analytical standard of AM6545 (HY-110206). This product is intended for research and analytical applications. AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications. | ||||||||||||||||||||
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References
- [1]. N L Cluny, et al. A novel peripherally restricted cannabinoid receptor antagonist, AM6545, reduces food intake and body weight, but does not cause malaise, in rodents. Br J Pharmacol. 2010 Oct;161(3):629-42. [Content Brief]
- [2]. Dalle S, Schouten M, Deboutte J, de Lange E, Ramaekers M, Koppo K. The molecular signature of the peripheral cannabinoid receptor 1 antagonist AM6545 in adipose, liver and muscle tissue. Toxicol Appl Pharmacol. 2024 Oct;491:117081. [Content Brief]
- [3]. Eid BG, Neamatallah T, Hanafy A, El-Bassossy HM, Binmahfouz L, Aldawsari HM, Hasan A, El-Aziz GA, Vemuri K, Makriyannis A. Interference with TGFβ1-Mediated Inflammation and Fibrosis Underlies Reno-Protective Effects of the CB1 Receptor Neutral Antagonists AM6545 and AM4113 in a Rat Model of Metabolic Syndrome. Molecules. 2021 Feb 6;26(4):866. doi: 10.3390/molecules26040866. Erratum in: Molecules. 2024 Feb 19;29(4):902. [Content Brief]
