A pyrrolidinecarbamate compound that acts as a specific REV-ERB-alpha/beta agonist. Exhibits a direct and reversible binding (Kd = 800nM 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 800nM in Gal4-REV-ERB-alpha and beta transfected HEK 293 cells) and reduces BMAL1 mRNA in HepG2 cells (IC50 = 710nM). Shown to cross the blood-brain barrier and exhibit desirable pharmacokinetic properties. A 7-day administration of SR9009 (100mg/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. 217739, CAS 1379686-30-2, acts as a specific REV-ERB-alpha/beta agonist that exhibits a direct and reversible binding (Kd = 800nM). Synonyms: Ethyl-3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)pyrrolidine-1-carboxylate CAS Number: 1379686-30-2 Molecular Weight: 437.9 Molecular Formula: C20H24ClN3O4S Solubility: DMSO Primary Target: REV-ERB-alpha/beta Appearance: Dark brown liquid. Purity: 96% (HPLC) Storage and Stability: Store at 4C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Molekulargewicht:
437.9
Reinheit:
96% (HPLC)
Formulierung:
Supplied as a dark brown liquid.
CAS Nummer:
[1379686-30-2]
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