REV-ERB Agonist II, SR9009-Calbiochem

C₂₀H₂₄ClN₃O₄S

437.94

MFCD29472236

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.

Cell permeable: yes
Primary Target
REV-ERB-α/&beta
Reversible: yes

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Solt, L.A., et al. 2012. Nature485, 62.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥96% (HPLC)

liquid

Calbiochem^®

OK to freeze
protect from light

dark brown

DMSO: 50 mg/mL

ambient

2-8℃

ClC(C=C1)=CC=C1CN(CC2=CC=C(S2)[N+]([O-])=O)CC3CN(C(OCC)=O)CC3

25 mg in Glass bottle
Packaged under inert gas

10 - Combustible liquids

WGK 3