S9576
SR8278
≥98% (HPLC)
Synonym(s):
1,2,3,4-Tetrahydro-2-[[5-(methylthio)-2-thienyl]carbonyl]-3-isoquinolinecarboxylic acid ethyl ester
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About This Item
Empirical Formula (Hill Notation):
C18H19NO3S2
CAS Number:
Molecular Weight:
361.48
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI key
UIEBLUZPSFAFOC-UHFFFAOYSA-N
SMILES string
CCOC(=O)C1Cc2ccccc2CN1C(=O)c3ccc(SC)s3
InChI
1S/C18H19NO3S2/c1-3-22-18(21)14-10-12-6-4-5-7-13(12)11-19(14)17(20)15-8-9-16(23-2)24-15/h4-9,14H,3,10-11H2,1-2H3
assay
≥98% (HPLC)
form
lyophilized powder
color
white
solubility
DMSO: ≥30 mg/mL
storage temp.
2-8°C
Quality Level
Application
SR8278 has been used as a nuclear receptor subfamily 1, group D, member 1 (NR1D1) antagonist to study its effects on starvation-induced macrophages.
SR8278 was used as rev-erb alpha antagonist to study the regulation of glucagon secretion in mouse pancreatic alpha cells1 and beta cells.2
Biochem/physiol Actions
SR8278 is a Nuclear Heme Receptor REV-ERB antagonist.
SR8278 is a Nuclear Heme Receptor REV-ERB antagonist. REV-ERBα plays a critical role in regulation of the circadian rhythm by repressing target gene activities. Additionally, REV-ERBα has been shown to regulate metabolic processes including lipid and glucose metabolism. SR8278 blocks the ability of the synthetic agonist GSK4112 to enhance REV-ERBα-dependent repression and stimulates the expression of REV-ERBα target genes involved in gluconeogenesis.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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NR1D1 ameliorates Mycobacterium tuberculosis clearance through regulation of autophagy
Chandra V, et al.
Autophagy, 11(11), 1987-1997 (2015)
Dapeng Yu et al.
International immunopharmacology, 73, 312-320 (2019-05-28)
Progressive lung injury and pulmonary inflammation can be induced by an intraperitoneal injection of lipopolysaccharide (LPS). Interleukin-1β (IL-1β) is a key pro-inflammatory cytokine that can further exaggerate inflammation, which is cleaved and activated by the NALP3 inflammasome. Although the nuclear
Elaine Vieira et al.
Endocrinology, 153(2), 592-601 (2011-12-15)
Disturbances of circadian rhythms have been associated with obesity and type 2 diabetes. The nuclear receptor Rev-erbα was suggested to link circadian rhythms and metabolism in peripheral tissues. The aim of the present study was to dissect the role of
Yihao Tian et al.
International journal of molecular medicine, 47(2), 633-642 (2021-01-09)
Melatonin, secreted in a typical diurnal rhythm pattern, has been reported to prevent osteoporosis; however, its role in osteoclastogenesis remains unclear. In the present study, the ability of melatonin to inhibit receptor activator of nuclear factor‑κB ligand (RANKL)‑induced osteoclastogenesis and
Elaine Vieira et al.
PloS one, 8(7), e69939-e69939 (2013-08-13)
Disruption of pancreatic clock genes impairs pancreatic beta-cell function, leading to the onset of diabetes. Despite the importance of pancreatic alpha-cells in the regulation of glucose homeostasis and in diabetes pathophysiology, nothing is known about the role of clock genes
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