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S9576

Sigma-Aldrich

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:
1254944-66-5
Molecular Weight:
361.48
MDL number:
MFCD18782736
UNSPSC Code:
12352200
PubChem Substance ID:
329824626
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. 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

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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
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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