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Merck
CN

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:
Assay:
≥98% (HPLC)
Form:
lyophilized powder
Quality level:
Technical Service
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Quality Level

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

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
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



Global Trade Item Number

SKUGTIN
S9576-25MG04061832824383
S9576-5MG04061832824390