SR9011 --- REV-ERB Agonist

Overview
Catalog #	bs-66049c-2-mg-solid
Product Name	SR9011 --- REV-ERB Agonist
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 479.04 Formula: C23 H31 Cl N4 O3 S CAS Number: 1379686-29-9 InChi Key: PPUYOYQTTWJTIU-UHFFFAOYSA-N InChi: InChI=1S/C23H31ClN4O3S/c1-2-3-4-12-25-23(29)27-13-11-19(16-27)15-26(14-18-5-7-20(24)8-6-18)17-21-9-10-22(32-21)28(30)31/h5-10,19H,2-4,11-17H2,1H3,(H,25,29) Smiles: CCCCCNC(=O)N1CC(CN(CC2C=CC(Cl)=CC=2)CC2=CC=C(S2)[N+]([O-])=O)CC1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	SR9011 is a potent and specific synthetic REV-ERB agonist that binds to REV-ERB-α with an EC50 ~790 nM and REV-ERB-β with EC50 ~560 nM. It also has good in vivo plasma/brain exposure. The nuclear receptors REV-ERB-α and REV-ERB-β play an integral role in regulating the expression of core clock proteins, driving rhythms in activity and metabolism. Administration of SR9011 alters circadian behavior and the circadian pattern of core clock gene expression in the hypothalami of mice. The circadian expression pattern of an array of metabolic genes in the liver, skeletal muscle and adipose tissue was also altered, resulting in increased energy expenditure. Treatment of diet-induced obese mice with SR9011 decreased obesity by reducing fat mass and markedly improved dyslipidaemia and hyperglycaemia. These results indicate that synthetic REV-ERB ligands that pharmacologically target the circadian rhythm may be beneficial in the treatment of sleep disorders as well as metabolic diseases.