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
- Molecular Weight:
- 361.48
- MDL Number:
- MFCD18782736
- MOL File:
- 1254944-66-5.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| SR8278 ≥98% (HPLC) | S9576 | 5mg | $187 |
| SR8278 ≥98% (HPLC) | S9576 | 25mg | $712 |
| SR8278 ≥90% | 17000 | 1mg | $49 |
| SR8278 ≥90% | 17000 | 5mg | $120 |
| SR8278 ≥90% | 17000 | 10mg | $222 |
| More product size | |||
| 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 |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SR8278 price More Price(62)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | S9576 | SR8278 ≥98% (HPLC) | 1254944-66-5 | 5mg | $187 | 2026-04-30 | Buy |
| Sigma-Aldrich | S9576 | SR8278 ≥98% (HPLC) | 1254944-66-5 | 25mg | $712 | 2026-04-30 | Buy |
| Cayman Chemical | 17000 | SR8278 ≥90% | 1254944-66-5 | 1mg | $49 | 2026-04-30 | Buy |
| Cayman Chemical | 17000 | SR8278 ≥90% | 1254944-66-5 | 5mg | $120 | 2026-04-30 | Buy |
| Cayman Chemical | 17000 | SR8278 ≥90% | 1254944-66-5 | 10mg | $222 | 2026-04-30 | Buy |
SR8278 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32466 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30225 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39039 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
| HANGZHOU LEAP CHEM CO., LTD. | +86-571-87711850 | market18@leapchem.com | China | 43333 | 58 |
| Shanghai Acmec Biochemical Technology Co., Ltd. | +86-18621343501; +undefined18621343501 | product@acmec-e.com | China | 33324 | 58 |
