An antagonist of REV-ERBα (EC50 = 0.47 µM)

SR8278 – 25 mg

Brand:
Cayman
CAS:
1254944-66-5
Storage:
-20
UN-No:
Non-Hazardous - /

REV-ERBα is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner.{27845,21477} SR8278 is an antagonist of REV-ERBα (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112 (Item No. 11931).{21477} Moreover, SR8278 stimulates the expression of two REV-ERBα target genes involved in the regulation of glucose production, glucose 6-phosphatase and phosphoenolpyruvate carboxykinase, in liver cells.{21477} SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells.{27844}  

 

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Description

An antagonist of REV-ERBα (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112; stimulates the expression of the REV-ERBα target genes G6Pase and PEPCK in liver cells; used to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells

Formal name: 1,2,3,4-tetrahydro-2-[[5-(methylthio)-2-thienyl]carbonyl]-3-isoquinolinecarboxylic acid, ethyl ester

Synonyms: 

Molecular weight: 361.5

CAS: 1254944-66-5

Purity: ≥90%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Neuroscience|Behavioral Neuroscience|Sleep & Biological Rhythms

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