1254944-66-5 Usage
Description
REV-ERBα is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner. SR8278 is an antagonist of REV-ERBα (EC50 = 0.47 μM), blocking activation of the receptor by the synthetic agonist GSK 4112 . 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. SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells.
Uses
SR 8278 is a synthetic antagonist of the nuclear heme receptor REV-ERB.
Check Digit Verification of cas no
The CAS Registry Mumber 1254944-66-5 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,5,4,9,4 and 4 respectively; the second part has 2 digits, 6 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1254944-66:
(9*1)+(8*2)+(7*5)+(6*4)+(5*9)+(4*4)+(3*4)+(2*6)+(1*6)=175
175 % 10 = 5
So 1254944-66-5 is a valid CAS Registry Number.
1254944-66-5Relevant articles and documents
MODULATORS OF REV-ERB
-
, (2015/07/16)
The subject matter herein concerns the identification and development of potent synthetic REV-ERB ligands, such as in vivo agonists and antagonists. These compounds allow for characterization of the effects of modulation of this receptor in vivo specifically on circadian behavior and metabolism, and have suitable characteristics for development of medicinal compounds useful for treatment of malconditions such as diabetes, obesity, atherosclerosis, dyslipidemia, a circadian rhythm disorder, coronary artery disease, bipolar disorder, depression, cancer, a sleep disorder, an anxiety disorder, an addiction disorder, a bone-related disorder such osteoporosis, a skeletal muscle disease, e.g., with compromised exercise capacity, or an autoimmune disorder such as psoriasis, multiple sclerosis, inflammatory bowel disease, and others.
