SR9011
Nome Químico: 3-[[[(4-chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-N-pentyl-1-pyrrolidinecarboxamide
Número CAS: 1379686-29-9
Fórmula química: C23H31ClN4O3S
Peso molecular: 479.0
Pureza: not less than 98%
Aparência: white or almost white crystalline powder.
Armazenar: Armazenar em temperatura ambiente, hermeticamente fechado, longe do calor, luz e umidade.
Inscrição： Modulador seletivo de receptor de andrógeno (SARMs)
SR9011 é um agonista sintético potente e específico de REV-ERB que se liga a REV-ERB-α com EC50 ~790 nM e REV-ERB-β com EC50 ~560 nM. Também tem boa exposição plasmática/cérebro in vivo. Os receptores nucleares REV-ERB-α e REV-ERB-β desempenham um papel fundamental na regulação da expressão das proteínas centrais do relógio, conduzindo ritmos na atividade e no metabolismo.
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
