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]
^Dodson B (2013-08-20). "New drug mimics the beneficial effects of exercise". Gizmag. Retrieved 2013-08-21.
^Solt LA, Wang Y, Banerjee S, Hughes T, Kojetin DJ, Lundasen T, et al. (March 2012). "Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists". Nature. 485 (7396): 62–68. Bibcode:2012Natur.485...62S. doi:10.1038/nature11030. PMC3343186. PMID 22460951.
^Dierickx P, Emmett MJ, Jiang C, Uehara K, Liu M, Adlanmerini M, Lazar MA (June 2019). "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. Bibcode:2019PNAS..11612147D. doi:10.1073/pnas.1904226116. PMC6589768. PMID 31127047.
^Woldt E, Sebti Y, Solt LA, Duhem C, Lancel S, Eeckhoute J, et al. (August 2013). "Rev-erb-α modulates skeletal muscle oxidative capacity by regulating mitochondrial biogenesis and autophagy". Nature Medicine. 19 (8): 1039–1046. doi:10.1038/nm.3213. PMC3737409. PMID 23852339.
^Mazzarino M, Rizzato N, Stacchini C, de la Torre X, Botrè F (November 2018). "A further insight into the metabolic profile of the nuclear receptor Rev-erb agonist, SR9009". Drug Testing and Analysis. 10 (11–12): 1670–1681. doi:10.1002/dta.2538. hdl:11573/1291262. PMID 30395700. S2CID 53223664.
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sr9009, also, known, stenabolic, research, drug, that, developed, professor, thomas, burris, scripps, research, institute, agonist, erba, increases, constitutive, repression, genes, regulated, erba, with, half, maximum, inhibitory, concentration, ic50, erbaα, . 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 ErbAa and IC50 800 nM for Rev ErbAb 2 In an animal study some of its effects were found to be independent of REV ERB with an unknown mechanism of action 3 SR9009IdentifiersIUPAC name ethyl 3 4 chlorobenzyl 5 nitrothiophen 2 yl methyl amino methyl pyrrolidine 1 carboxylateCAS Number1379686 30 2PubChem CID57394020ChemSpider28487410UNIIX5DCA09N30ChEMBLChEMBL1961796Chemical and physical dataFormulaC 20H 24Cl N 3O 4SMolar mass437 94 g mol 13D model JSmol Interactive imageSMILES CCOC O N1CCC C1 CN CC2 CC C C C2 Cl CC3 CC C S3 N O O InChI InChI 1S C20H24ClN3O4S c1 2 28 20 25 23 10 9 16 13 23 12 22 11 15 3 5 17 21 6 4 15 14 18 7 8 19 29 18 24 26 27 h3 8 16H 2 9 14H2 1H3Key MMJJNHOIVCGAAP UHFFFAOYSA NActivation of Rev ErbA a 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 editGSK4112 GW501516 SR8278 SR9011References edit Dodson B 2013 08 20 New drug mimics the beneficial effects of exercise Gizmag Retrieved 2013 08 21 Solt LA Wang Y Banerjee S Hughes T Kojetin DJ Lundasen T et al March 2012 Regulation of circadian behaviour and metabolism by synthetic REV ERB agonists Nature 485 7396 62 68 Bibcode 2012Natur 485 62S doi 10 1038 nature11030 PMC 3343186 PMID 22460951 Dierickx P Emmett MJ Jiang C Uehara K Liu M Adlanmerini M Lazar MA June 2019 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 Bibcode 2019PNAS 11612147D doi 10 1073 pnas 1904226116 PMC 6589768 PMID 31127047 Woldt E Sebti Y Solt LA Duhem C Lancel S Eeckhoute J et al August 2013 Rev erb a modulates skeletal muscle oxidative capacity by regulating mitochondrial biogenesis and autophagy Nature Medicine 19 8 1039 1046 doi 10 1038 nm 3213 PMC 3737409 PMID 23852339 Prohibited List 2014 07 22 Mazzarino M Rizzato N Stacchini C de la Torre X Botre F November 2018 A further insight into the metabolic profile of the nuclear receptor Rev erb agonist SR9009 Drug Testing and Analysis 10 11 12 1670 1681 doi 10 1002 dta 2538 hdl 11573 1291262 PMID 30395700 S2CID 53223664 nbsp This pharmacology related article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title SR9009 amp oldid 1215440675, wikipedia, wiki, book, books, library,
