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S9576

Sigma-Aldrich

SR8278

≥98% (HPLC)

Synonyme(s) :

1,2,3,4-Tetrahydro-2-[[5-(methylthio)-2-thienyl]carbonyl]-3-isoquinolinecarboxylic acid ethyl ester

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About This Item

Formule empirique (notation de Hill):
C18H19NO3S2
Numéro CAS:
1254944-66-5
Poids moléculaire :
361.48
Numéro MDL:
MFCD18782736
Code UNSPSC :
12352200
ID de substance PubChem :
329824626
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

lyophilized powder

Couleur

white

Solubilité

DMSO: ≥30 mg/mL

Température de stockage

2-8°C

Chaîne SMILES 

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

Clé InChI

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

Actions biochimiques/physiologiques

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.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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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
NR1D1 ameliorates Mycobacterium tuberculosis clearance through regulation of autophagy
Chandra V, et al.
Autophagy, 11(11), 1987-1997 (2015)
Johanna Ndikung et al.
Environment international, 134, 105265-105265 (2019-11-18)
The growing requirement of hazard and risk assessment of environmental chemicals and the efforts to minimize animal testing, increases the demand for innovative and predictive in vitro test systems in toxicology, reflecting the physiological conditions of human nature. Here, an
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
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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