REV-ERB Agonist II, SR9009 – Calbiochem

Descrição detalhada : A pyrrolidinecarbamate compound that acts as a specific REV-ERB-alpha/beta agonist. Exhibits a direct and reversible binding (Kd = 800 nM REV-ERB-alpha) and shows excellent selectivity over a panel of 46 other nuclear receptors. Potently increases REV-ERB-dependent repressor activity (IC50 = 670 and 800 nM in Gal4-REV-ERB-alpha and beta transfected HEK 293 cells) and reduces BMAL1 mRNA in HepG2 cells (IC50 = 710 nM). Shown to cross the blood-brain barrier and exhibit desirable pharmacokinetic properties. A 7-day administration of SR9009 (100 mg/kg, i.p., b.i.d.) causes a significant weight and fat loss in C57BL6 mice with concomitant reduction in plasma glucose and free fatty acid levels, and alters circadian pattern.
Sinónimos : REV-ERB Agonist II, SR9009 - Calbiochem; Ethyl-3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)pyrrolidine-1-carboxylate
Fórmula molecula r: C20H24ClN3O4S
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X25MG