Stenabolic (SR9009)

Cat# M5143-10mg

Size : 10mg

Brand : AbMole Bioscience

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Stenabolic (SR9009) Structure
Synonym:

Stenabolic; REV-ERB Agonist II


Quality Control & Documentation
Biological Activity

Stenabolic (SR9009) is an agonist of REV-ERB, with IC50 of 670 nM and 800 nM for REV-ERBα and REV-ERBβ respectively. Stenabolic (SR9009) inhibits the activity of the SCN clock, with reversible inhibition of circadian oscillations in SCN explants cultured from the Per2:luc reporter mouse. Stenabolic (SR9009) dose-dependently increases the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimeric Gal4 DNA Binding Domain (DBD) - REV-ERB ligand binding domain (LBD) α or β and a Gal4-responsive luciferase reporter. Stenabolic (SR9009) potently and efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the Bmal1 promoter (SR9009 IC50=710 nM).

Customer Product Validations & Biological Datas
Source Cell Physiol Biochem (2018). Figure 4. SR9009
Method MTT assay
Cell Lines The human monocytic leukemia cell line
Concentrations 1, 5, 10, and 50 µM
Incubation Time 12 h
Results Expression of hMMP-9 mRNA also decreased when cells were treated with SR9009 alone, without Ang II stimulation (P < 0.05). The effect of SR9009 was further confirmed on mouse MMP-9 (mMMP-9) mRNA expression in RAW264.7 macrophages
Protocol (for reference only)
Cell Experiment
Cell lines L929 cell
Preparation method Cells were treated with 100 ng/ml IFNg (Millipore) and 10 ng/ml LPS(Millipore) for M1 polarization. M2 differentiation was induced by incubating macrophages with 15 ng/ml IL-4 (Millipore).
Concentrations 10 μM
Incubation time 24 h
Animal Experiment
Animal models homozygous LDL receptor deficient (ldlr−/−) male mice
Formulation PBS
Dosages 100 mg/kg
Administration
Chemical Information
Molecular Weight 437.94
Formula C20H24ClN3O4S
CAS Number 1379686-30-2
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Geldof L, et al. Int J Mol Sci. In Vitro Metabolic Studies of REV-ERB Agonists SR9009 and SR9011.

[2] Solt LA, et al. Nature. Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.