REV-ERB Agonist II, SR9009, The REV-ERB Agonist II, SR9009 controls the biological activity of REV-ERB. This small molecule/inhibitor is primarily used for Biochemicals applications.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target REV-ERB-α/&beta
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Solt, L.A., et al. 2012. Nature485, 62.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
10 - Combustible liquids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Rev-erbα represents a powerful transcriptional repressor involved in immunity. However, the regulation, function, and clinical relevance of Rev-erbα in Helicobacter pylori infection are presently unknown. Rev-erbα was examined in gastric samples from H pylori-infected patients and mice. Gastric epithelial cells (GECs)
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