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
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
Assay
≥98% (HPLC)
form
lyophilized powder
color
white
solubility
DMSO: ≥30 mg/mL
storage temp.
2-8°C
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
InChI key
UIEBLUZPSFAFOC-UHFFFAOYSA-N
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 Code
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)
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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
Lianxia Guo et al.
British journal of pharmacology, 178(2), 328-345 (2020-10-18)
Acute kidney injury (AKI) is a common and critical illness, resulting in severe morbidity and a high mortality. There is a considerable interest in identifying novel molecular targets for management of AKI. We investigated the potential role of the circadian
Ryan D Welch et al.
Scientific reports, 7(1), 17142-17142 (2017-12-08)
Duchenne muscular dystrophy (DMD) is a debilitating X-linked disorder that is fatal. DMD patients lack the expression of the structural protein dystrophin caused by mutations within the DMD gene. The absence of functional dystrophin protein results in excessive damage from
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
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