REV-ERB AGONIST II SR9009 - CALBIOCHEM

General description

A pyrrolidinecarbamate compound that acts as a specific REV-ERB-α/β agonist. Exhibits a direct and reversible binding (K_d = 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