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554726  REV-ERB Agonist II, SR9009

Ethyl-3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)pyrrolidine-1-carboxylate

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18 April 2014

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A pyrrolidinecarbamate compound that acts as a specific REV-ERB-α/β agonist. Exhibits a direct and reversible binding (Kd = 800 nM REV-ERB-α) 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-α and β 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.
Product information
Form Dark brown liquid
Primary Target REV-ERB-α/&beta
Molar mass 437.9
Protect from Light Yes
Packaged under inert gas Yes
Cell permeable Yes
Reversible Yes
Purity ≥96% by HPLC
Solubility DMSO
Store and ship information
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling
REV-ERB Agonist II, SR9009, molecular structure

© Merck KGaA, Darmstadt, Germany, 2014

All references to Merck refer to Merck KGaA, Darmstadt, Germany.


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