SR8278

Product Name: SR8278
CAS No.: 1254944-66-5
Chemical Name: SR8278
Synonyms: SR8278;SR8278, 10 mM in DMSO;SR8278;SR-8278;SR 8278;UIEBLUZPSFAFOC-UHFFFAOYSA-N;SR-8278, REV-ERBalpha antagonist;ethyl2-(5-methylsulfanylthiophene-2-carbonyl)-3,4-dihydro-1H-isoquinoline-3-carboxylate;Ethyl 1,2,3,4-tetrahydro-2-[[5-(methylthio)-2-thienyl]carbonyl]-3-isoquinolinecarboxylate;Ethyl 2-(5-(methylthio)thiophene-2-carbonyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate;1,2,3,4-Tetrahydro-2-[[5-(methylthio)-2-thienyl]carbonyl]-3-isoquinolinecarboxylic acid ethyl ester;3-Isoquinolinecarboxylic acid, 1,2,3,4-tetrahydro-2-[[5-(methylthio)-2-thienyl]carbonyl]-, ethyl ester
CBNumber: CB42628428
Molecular Formula: C18H19NO3S2
Formula Weight: 361.48
MOL File: 1254944-66-5.mol

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SR8278 Property

Melting point:: 52-55°C
Boiling point:: 535.7±50.0 °C(Predicted)
Density: 1.32±0.1 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: DMSO: ≥30mg/mL
pka: -3.20±0.40(Predicted)
form: film
color: white to tan

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Safety

WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: S9576
Product name: SR8278
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $165.3
Updated: 2025/07/31

Sigma-Aldrich

Product number: S9576
Product name: SR8278
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $664
Updated: 2025/07/31

Cayman Chemical

Product number: 17000
Product name: SR8278
Purity: ≥90%
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 17000
Product name: SR8278
Purity: ≥90%
Packaging: 5mg
Price: $109
Updated: 2024/03/01

Cayman Chemical

Product number: 17000
Product name: SR8278
Purity: ≥90%
Packaging: 10mg
Price: $201
Updated: 2024/03/01

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SR8278 Chemical Properties,Usage,Production

Description

REV-ERBα is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner. SR8278 is an antagonist of REV-ERBα (EC₅₀ = 0.47 μM), blocking activation of the receptor by the synthetic agonist GSK 4112 . Moreover, SR8278 stimulates the expression of two REV-ERBα target genes involved in the regulation of glucose production, glucose 6-phosphatase and phosphoenolpyruvate carboxykinase, in liver cells. SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells.

Uses

SR 8278 is a synthetic antagonist of the nuclear heme receptor REV-ERB.

in vivo

SR8278 (slow microinjection; 20 μg/mouse) exerts antidepressant and anxiolytic effects in a circadian time-dependent manner in 6-OHDA-lesioned mice and restores the circadian rhythm of mood-related behaviors^[1].
? ? SR8278 (slow microinjection; 20 μg/mouse) restores the binding activities of REV-ERBα and NURR1 to the tyrosine hydroxylase promoter and the induction of enrichment of the R/N motif, recognized by REV-ERBα and NURR1^[1].

Animal Model:	6-OHDA-lesioned mice^[1]
Dosage:	20 μg/mouse
Administration:	slow microinjection; 20 μg/mouse
Result:	Recovered mood-related behavioral deficits shown in 6-OHDA-lesioned mice. Altered remaining DAergic neuron specific transcription levels of REV-ERBα and Nurr1 in the VTA. Restored antagonistic crosstalk of REV-ERBα and NURR1 binding activity to TH promoter and TH protein levels in VTA. Induced enrichments of REV-ERBα and NURR1 binding motifs at dawn.

storage

Store at +4°C

References

[1] HéLèNE DUEZ Bart S. Rev-erb-alpha: an integrator of circadian rhythms and metabolism.[J]. Journal of applied physiology, 2009, 107 6: 1972-1980. DOI: 10.1152/japplphysiol.00570.2009
[2] DOUGLAS KOJETIN. Identification of SR8278, a Synthetic Antagonist of the Nuclear Heme Receptor REV-ERB[J]. ACS Chemical Biology, 2010, 6 2: 131-134. DOI: 10.1021/cb1002575
[3] ELAINE VIEIRA. Involvement of the clock gene Rev-erb alpha in the regulation of glucagon secretion in pancreatic alpha-cells.[J]. PLoS ONE, 2013: e69939. DOI: 10.1371/journal.pone.0069939

SR8278 Preparation Products And Raw materials

Raw materials

Preparation Products

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SR8278 Suppliers

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1254944-66-5, SR8278Related Search:

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SR8278

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

UIEBLUZPSFAFOC-UHFFFAOYSA-N

SR8278;SR-8278;SR 8278

ethyl2-(5-methylsulfanylthiophene-2-carbonyl)-3,4-dihydro-1H-isoquinoline-3-carboxylate

Ethyl 1,2,3,4-tetrahydro-2-[[5-(methylthio)-2-thienyl]carbonyl]-3-isoquinolinecarboxylate

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

Duchenne muscular dystrophy,inhibit,metabolism,biological rhythm,Alzheimer's disease,SR-8278,SR8278,neurosurgery,Inhibitor,REV-ERBα,SR 8278,REV-ERB

Ethyl 2-(5-(methylthio)thiophene-2-carbonyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate

SR-8278, REV-ERBalpha antagonist

SR8278, 10 mM in DMSO

1254944-66-5

125944-66-5

123456