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. Solubility:DMSOPrimary Target:REV-ERB-alpha/betaMolar Mass:437.9Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
产品形式
该产品为深褐色液体。
保存建议
接收到REV-ERB Agonist II, SR9009 (Ethyl-3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)pyrrolidine-1-carboxylate)产品后，置于4°C温度下保存。
