Chemistry:SR9009

From HandWiki
Short description: Chemica compound, Agonist of Rev-ErbA
SR9009
SR9009 structure.svg
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC20H24ClN3O4S
Molar mass437.94026 g·mol−1
3D model (JSmol)

SR9009, also known as Stenabolic, is a research drug that was developed by professor Thomas Burris of the Scripps Research Institute as an agonist of Rev-ErbA (i.e., increases the constitutive repression of genes regulated by Rev-ErbA)[1] with a half-maximum inhibitory concentration (IC50) = 670 nM for Rev-ErbAα and IC50 = 800 nM for Rev-ErbAβ.[2] In an animal study, some of its effects were found to be independent of REV-ERB with an unknown mechanism of action.[3]

Activation of Rev-ErbA-α by SR9009 in mice increases exercise capacity by increasing mitochondria counts in skeletal muscle.[4]

Abuse of SR9009 has been reported within the bodybuilding community, resulting in SR9009 being placed on the World Anti-Doping Agency list of prohibited drugs. SR9009 and the related SR9011 drug are described as "Hormone and Metabolic Modulators".[5][6]

See also

References

  1. Dodson B (2013-08-20). "New drug mimics the beneficial effects of exercise". http://www.gizmag.com/scripps-drug-sr9009-exercise-mimic/28651/. 
  2. "Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists". Nature 485 (7396): 62–68. March 2012. doi:10.1038/nature11030. PMID 22460951. Bibcode2012Natur.485...62S. 
  3. "SR9009 has REV-ERB-independent effects on cell proliferation and metabolism". Proceedings of the National Academy of Sciences of the United States of America 116 (25): 12147–12152. June 2019. doi:10.1073/pnas.1904226116. PMID 31127047. Bibcode2019PNAS..11612147D. 
  4. "Rev-erb-α modulates skeletal muscle oxidative capacity by regulating mitochondrial biogenesis and autophagy". Nature Medicine 19 (8): 1039–1046. August 2013. doi:10.1038/nm.3213. PMID 23852339. 
  5. "Prohibited List". 2014-07-22. https://www.wada-ama.org/en/resources/science-medicine/prohibited-list-documents. 
  6. "A further insight into the metabolic profile of the nuclear receptor Rev-erb agonist, SR9009". Drug Testing and Analysis 10 (11–12): 1670–1681. November 2018. doi:10.1002/dta.2538. PMID 30395700.