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SR9009

Catalog No. T3685   CAS 1379686-30-2
Synonyms: Stenabolic, REV-ERB Agonist II

SR9009 (Stenabolic), a REV-ERB agonist, increases the constitutive repression of genes regulated by REV-ERBα/ERBβ (IC50: 670/800 nM). Through activation of REV-ERB, SR9009 can decrease circadian locomotor activity during the dark phase and alter the expression pattern of core clock genes in the hypothalami of mice. The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle, and adipose tissue was also altered in mice exposed to SR9009, resulting in increased energy expenditure. In Diet-induced obese mice, SR9009 (100 mg/kg, i.p., b.i.d., for 30 days) could decrease fat mass and markedly improve dyslipidemia and hyperglycemia.

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SR9009 Chemical Structure
SR9009, CAS 1379686-30-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 48.00
5 mg In stock $ 63.00
10 mg In stock $ 98.00
25 mg In stock $ 162.00
50 mg In stock $ 288.00
100 mg In stock $ 466.00
500 mg In stock $ 1,070.00
1 mL * 10 mM (in DMSO) In stock $ 63.00
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Purity: 99.8%
Purity: 99.53%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SR9009 (Stenabolic), a REV-ERB agonist, increases the constitutive repression of genes regulated by REV-ERBα/ERBβ (IC50: 670/800 nM). Through activation of REV-ERB, SR9009 can decrease circadian locomotor activity during the dark phase and alter the expression pattern of core clock genes in the hypothalami of mice. The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle, and adipose tissue was also altered in mice exposed to SR9009, resulting in increased energy expenditure. In Diet-induced obese mice, SR9009 (100 mg/kg, i.p., b.i.d., for 30 days) could decrease fat mass and markedly improve dyslipidemia and hyperglycemia.
Targets&IC50 REV-ERB-α:670 nM, REV-ERB-β:800 nM
In vitro SR9009 effectively inhibits transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the Bmal1 promoter (SR9009 IC50: 710 nM). SR9009 suppresses the expression of BMAL1 mRNA in HepG2 cells in a REV-ERBα/β-dependent manner.
In vivo SR9009 inhibits the activity of the SCN clock, with reversible inhibition of circadian oscillations in SCN explants cultured from the Per2: Luc reporter mouse.
Cell Research SR9009 is dissolved in DMSO and diluted with appropriate media[1]. HEK293 cells are grown in 96-well plates (1×106/well) and are transiently transfected using Lipofectamine. Cells are transfected with a total of 200 ng of DNA per well consisting of the pGL4 mIL-17 firefly luciferase reporter construct, the pGL4 mIL-17 + CNS-5 firefly luciferase reporter construct, or the pGL4 mIL-17 2kB RORE mutant (100 ng/well) , an actin promoter Renilla reniformis luciferase reporter (50 ng/well), and either control vector alone or the test DNA (full-length RORα or full-length RORγ at 50 ng/well). All 48 human nuclear receptors are represented in the specificity assay and SR9009 is tested at a concentration of 20 μM. The format of the assay is a cotransfection assay with Gal4 DNA binding domain-nuclear receptor fusions in HEK293 cells[1].
Synonyms Stenabolic, REV-ERB Agonist II
Molecular Weight 437.94
Formula C20H24ClN3O4S
CAS No. 1379686-30-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 43.8 mg/mL(100 mM)

TargetMolReferences and Literature

1. Solt LA, et al. Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. Nature. 2012 Mar 29;485(7396):62-68.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Compound Library NO PAINS Compound Library Preclinical Compound Library Inhibitor Library Autophagy Compound Library

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Keywords

SR9009 1379686-30-2 Autophagy Inhibitor inhibit Stenabolic SR 9009 REV-ERB Agonist II SR-9009 inhibitor

 

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