SR9009

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SR9009
SR9009 structure.svg
Identifiers
CAS Number
PubChem CID
ChemSpider
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]

Activation of Rev-ErbA-α by SR9009 in mice increases exercise capacity by increasing mitochondria counts in skeletal muscle.[3]

Human Use[edit]

Some companies are selling SR9009 online for human use as a 'research chemical.' In an email correspondence, the developer, Prof. Burris said of SR9009's use in humans: "I just recently found out that someone is selling SR9009 in a manner that is "supported" for human use in bodybuilding. I agree with your comments. The drug does in fact alter the circadian rhythm (in mice) and we would need to assume in humans – and we don't know if it is beneficial or detrimental at this point. SR9009 was designed as a "tool" molecule to determine if we should pursue making more drug like compounds that could be used to treat disease. Of course, the data is supportive of going forward – and we are designing better compounds – but the issue is that SR9009 has several issues that make it unsuitable for human use. Firstly, it has no oral bioavailability. I know the company selling this is indicating taking it orally is ok – but it doesn't even get into the blood. At this point that is probably not a bad thing since the drug has not been evaluated in appropriate toxicology assays to determine if there are issues like inducing disease (cancer as you indicate or others). There is going to be exposure to the gut and that is not necessarily good since we don't know the effects as of yet. SR9009 has some functional groups that are known to have potential toxicology liabilities and it would never be developed as a drug. It was ok as a "tool" to figure out if we should continue to spend money and effort to get better drugs – but we had to design these "bad" functional groups out since they are know to have toxic effects in humans. So bottom line – I would never recommend using this compound at this point. That being said – we are still working on improved compounds with one of the potential uses being sarcopenia – loss of muscle and strength due to aging."[4]

SR9009 is currently on the World Anti-Doping Association list of prohibited drugs. [5]

See also[edit]

References[edit]

  1. ^ Dodson B (2013-08-20). "New drug mimics the beneficial effects of exercise". Health and Wellbeing. Gizmag. Retrieved 2013-08-21.
  2. ^ Solt LA; Wang Y; Banerjee S; Hughes T; Kojetin DJ; Lundasen T; Shin Y; Liu J; Cameron MD; Noel R; Yoo SH; Takahashi JS; Butler AA; Kamenecka TM; Burris TP (May 2012). "Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists". Nature. 485 (7396): 62–8. doi:10.1038/nature11030. PMC 3343186. PMID 22460951. Lay summaryNature Magazine.
  3. ^ Woldt E; Sebti Y; Solt LA; Duhem C; Lancel S; Eeckhoute J; Hesselink MK; Paquet C; Delhaye S; Shin Y; Kamenecka TM; Schaart G; Lefebvre P; Nevière R; Burris TP; Schrauwen P; Staels B; Duez H (August 2013). "Rev-erb-α modulates skeletal muscle oxidative capacity by regulating mitochondrial biogenesis and autophagy". Nat. Med. 19 (8): 1039–46. doi:10.1038/nm.3213. PMC 3737409. PMID 23852339. Lay summaryVoice of America (2013-07-19).
  4. ^ https://www.reddit.com/r/Nootropics/comments/2vtrjq/comment/ctksxv1. Missing or empty |title= (help)
  5. ^ "Prohibited List".