SR8278
SR8278 Basic information
- 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
- 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
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. |
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
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