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AM251 is a cannabinoid receptor 1 (CB1) antagonist/inverse agonist. It works by inhibiting the action of the endocannabinoid system. AM251 shows beneficial effects as an anti-obesity compound. AM251 is renal-protective in rats fed a high-fat diet. Also, AM251 decreases expression of estrogen-related receptor alpha (EER α), a potential therapeutic target for obesity. AM251 also show beneficial effects for the impairment of fear memory in rats.
| Cas No. | 183232-66-8 |
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| Purity | ≥97% |
| Formula | C22H21Cl2IN4O |
| Formula Wt. | 555.24 |
| Chemical Name | 1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide |
| IUPAC Name | 1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide |
| Synonym | AM-251, AM 251 |
| Solubility | 25mM in ethanol 100mM in DMSO |
| Appearance | White powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
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| Info Sheet |
Krzysik-Walker SM, Gonzalez-Mariscal I, Scheibye-Knudsen M, et al. The Biarylpyrazole Compound AM251 Alters Mitochondrial Physiology via Proteolytic Degradation of ERRalpha. Mol. Pharm. 2013. 83:157-166. PMID: 23066093.
Ratano P, Everitt BJ and Milton AL. The CB1 Receptor Antagonis AM251 Impairs Reconsolidation of Pavlovian Fear Memory in the Rat Basolateral Amygdala. Neuropsychopharmoacology. 2014 Oct;39(11):2529-37. PMID: 24801769.
Jenkin KA, O’Keefe L, Simcocks AC, et al. Chronic administration of AM251 improves albuminuria and renal tubular structure in obese rats. J Endocrin. 2015 May;225(2)113-24. PMID: 25804605.