SR9011
Nom chimique: 3-[[[(4-chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-N-pentyl-1-pyrrolidinecarboxamide
Numero CAS: 1379686-29-9
Chemical Formula: C23H31ClN4O3S
Masse moléculaire: 479.0
Pureté: not less than 98%
Apparence: white or almost white crystalline powder.
Stockage: Store at room temperature, tightly sealed, away from heat, light and moisture.
Application： Selective Androgen Receptor Modulator (SARM)
SR9011 is a potent and specific synthetic REV-ERB agonist that binds to REV-ERB-α with an EC50 ~790 nM and REV-ERB-β with EC50 ~560 nM. It also has good in vivo plasma/brain exposure. The nuclear receptors REV-ERB-α and REV-ERB-β play an integral role in regulating the expression of core clock proteins, driving rhythms in activity and metabolism.
Administration of SR9011 alters circadian behavior and the circadian pattern of core clock gene expression in the hypothalami of mice. The circadian expression pattern of an array of metabolic genes in the liver, skeletal muscle and adipose tissue was also altered, resulting in increased energy expenditure.
Treatment of diet-induced obese mice with SR9011 decreased obesity by reducing fat mass and markedly improved dyslipidaemia and hyperglycaemia. These results indicate that synthetic REV-ERB ligands that pharmacologically target the circadian rhythm may be beneficial in the treatment of sleep disorders as well as metabolic
