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SR9009

SR9009 20mg/2ml vial

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SR9009

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SR9009
Rating: 5 out of 2 reviews
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SR9009. Investigational name: SR9009

SR9009 profile:

Physiological processes involving metabolism and behaviour, e.g., activity/rest, are generally organised on a cycle of approximately 24 hours driven by a circadian rhythm.1 Disruption in circadian behaviours, particularly sleep, is associated with negative health outcomes. Insufficient sleep contributes to obesity, diabetes, cardiovascular disease, and decreased alertness and memory.1,2 In a recent study, patients exposed to one week of insufficient sleep (5.7 ±0.03 h) revealed up and down regulated genes, including those involved in the circadian rhythm, sleep homeostasis, oxidative stress and metabolism, which highlights the crosstalk between sleep and metabolism.2

The nuclear receptors reversed-viral erythroblastosis α and β (REV-ERB α and β) regulate the expression of core clock proteins and therefore modulate the circadian rhythm.1 Like most nuclear receptors, the REV-ERBs are ligand-dependent transcription factors and considerable progress has been made identifying both endogenous and synthetic ligands specific for these NRs.3 The number of compounds that have been developed to target components of the circadian molecular clock is very limited and of those there is even less data available demonstrating a clear therapeutic value for these types of compounds at this point.4 SR9009 is a Rev-ErbA ligand, developed by Prof. Thomas Burris of the Scripps Research Institute.

Recently, the REV-ERBα and REV-ERBβ (NR1D1 and NR1D2, respectively) have received considerable attention due to their integral roles in regulation of the core clock proteins. In fact, REV-ERBs have been proposed as core clock proteins since mice lacking both REV-ERBα and REV-ERBβ lack a circadian rhythm.4

To investigate the usefulness of REV-ERB agonists to affect sleep characteristics, SR9009 was administered in several experiments to test short-term tolerance, efficacy, and optimal time points in which it would remain effective.4 Results from these studies suggested that REV-ERB agonists may be useful in aiding the maintenance of wakefulness in pathological conditions affecting sleep.1,2,4

SR9009 in particular, was able to induce wakefulness at different times during the light period and showed no short-term tolerance development while maintaining its efficacy when administered repeatedly throughout the rodent’s inactive period.4 When SR9009 was administered at the time of peak REV-ERB mRNA expression, increased wakefulness for the first 2-3hrs immediately after injection was observed in several EEG studies in mice. Recent experiments have also demonstrated that REV-ERB agonists not only induce wakefulness and reduce sleep, but the compounds are also effective as anxiolytic agents.4

Modulation of the REV-ERB activity by synthetic agonists, like SR9009 also alters the expression of genes involved in lipid and glucose metabolism and, therefore, plays an important role in maintaining the energy homeostasis.1 Effects of SR9009 observed via in vitro and in vivo animal studies include increased basal oxygen consumption; decreased cholesterol and bile acid synthesis in the liver, and reduced lipogenesis; increased mitochondrial content, glucose and fatty acid oxidation in the skeletal muscle as well as decreased lipid storage in the white adipose.1 The recorded increase in energy expenditure and decrease in fat mass make the REV-ERB agonist SR9009 a promising candidate for the treatment of numerous metabolic disorders. Moreover, the increase in exercise capacity observed via in vivo animal studies makes it attractive for performance enhancement.1

REV-ERBs have been demonstrated to play important roles in regulation of immune function as well; these receptors have been shown to regulate the expression of inflammatory cytokines interleukin-6 and Ccl2; REVERBα is expressed in macrophages found in human atherosclerotic lesions.3 A recent study demonstrates that hematopoetic knock down of REV-ERBα can increase atherosclerosis in LDLR null mice providing clear evidence that REV-ERB plays a role in atherosclerosis.5 Furthermore, use of SR9009 in atherosclerotic mice resulted in gain of REV-ERB function and reduced atherosclerosis. Also, when mice were treated with SR9009 twice a day, significant effects on plasma lipid levels were observed.3 Such findings suggest that REV-ERBα has anti-atherogenic function and may represent a novel target for prevention and treatment of atherosclerosis.3

SR9009 is manufactured by SynTech Biochem, China, and contains synthetic SR9009 in a liquid formulation. SR9009 comes in a single 20mg/2ml SR9009 vial.

Description:

Formula: C20H24ClN3O4S
Mol. Weight: 437.94 g/mol

Molecular Structure:

 SR9009

Synonyms:

SR 9009, SR-9009, Stenabolic.

Physical Appearance

Liquid.

Specificity:

SR9009 is a Rev-ErbA ligand. Rev-ErbA is a member of the nuclear receptor family of intracellular transcription factors.

Purity:

≥98% (HPLC analysed).

Stability:

Store liquid formulation at 4 °C. The liquid formulated compound remains stable until the expiry date when stored at 4 °C..

Source:

Chemical Synthesis

Usage:

Product is prepared for LABORATORY RESEARCH USE ONLY. The product may not be used for other purposes.

References:

  1. Geldof, Lore et al. “In Vitro Metabolic Studies of REV-ERB Agonists SR9009 and SR9011.” Ed. Chang Won Choi. International Journal of Molecular Sciences 17.10 (2016):1676.
  2. Möller-Levet, Carla S. et al. “Effects of Insufficient Sleep on Circadian Rhythmicity and Expression Amplitude of the Human Blood Transcriptome.” Proceedings of the National Academy of Sciences of the United States of America 110.12 (2013): E1132–E1141.
  3. Sitaula, Sadichha et al. “Suppression of Atherosclerosis by Synthetic REV-ERB Agonist.” Biochemical and biophysical research communications 460.3 (2015):566–571.
  4. Amador, Ariadna et al. “Pharmacological Targeting the REV-ERBs in Sleep/Wake Regulation.” Ed. Nicolas Cermakian. PLoS ONE 11.9 (2016):e0162452.
  5. Ma H, et al.Increased atherosclerotic lesions in LDL receptor deficient mice with hematopoietic nuclear receptor Rev-erbα knock- down.” J Am Heart Assoc. 2013;2:e000235.



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igor

05/15/2017
5
James

Any help on dosage?

 
James

03/27/2017
5
Finally a great source for SR9009

Finally found a good reliable, helpful, supplier to buy SR9009. You have a customer for a very long time now DRS-labs, thank you

 
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