- SR8278
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- $42.00
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2026-05-11
- CAS:1254944-66-5
- Purity: 99.73%
- Supply Ability: 10g
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| Product Name: | SR8278 | | Synonyms: | 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 | | CAS: | 1254944-66-5 | | MF: | C18H19NO3S2 | | MW: | 361.48 | | EINECS: | | | Product Categories: | 123456 | | Mol File: | 1254944-66-5.mol |  |
| | SR8278 Chemical Properties |
| 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 | | 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 | | InChIKey | UIEBLUZPSFAFOC-UHFFFAOYSA-N | | SMILES | CCOC(=O)C1Cc2ccccc2CN1C(=O)c3ccc(SC)s3 |
| WGK Germany | 3 | | Storage Class | 11 - Combustible Solids |
| | SR8278 Usage And Synthesis |
| 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.
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| | 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 |
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