bs-60236C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 474.4

Formula: C20 H25 Cl2 N3 O4 S

CAS Number: 1379686-30-2

InChi Key: IXPPNWYUDXZKRX-UHFFFAOYSA-N

InChi: InChI=1S/C20H24ClN3O4S.ClH/c1-2-28-20(25)23-10-9-16(13-23)12-22(11-15-3-5-17(21)6-4-15)14-18-7-8-19(29-18)24(26)27;/h3-8,16H,2,9-14H2,1H3;1H

Smiles: Cl.CCOC(=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:

SR9009 is a potent and specific synthetic REV-ERB agonist that binds to REV-ERB-α with an EC50 ~670 nM and REV-ERB-β with EC50 ~800 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 SR9009 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 SR9009 decreased obesity by reducing fat mass and markedly improved dyslipidaemia and hyperglycaemia. It improves muscle mitochondrial function too. 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.