SR9011

SR9011 is a research drug that was developed by Professor Thomas Burris of Scripps as an agonist of Rev-ErbAα with a half-maximum inhibitory concentration (IC50) = 790 nM for Rev-Erbα and IC50 = 560 nM for Rev-ErbAβ.[1] It has been used in the study of the regulation of the circadian rhythm and its links to immune system function, inflammation and cancer.[2][3][4][5][6][7]

SR9011
Identifiers
IUPAC name
  • 3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)-N-pentylpyrrolidine-1-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC23H31ClN4O3S
Molar mass479.04 g·mol−1
3D model (JSmol)
SMILES
  • CCCCCNC(=O)N1CCC(CN(Cc2ccc(Cl)cc2)Cc3ccc(s3)[N+](=O)[O-])C1
InChI
  • InChI=1S/C23H31ClN4O3S/c1-2-3-4-12-25-23(29)27-13-11-19(16-27)15-26(14-18-5-7-20(24)8-6-18)17-21-9-10-22(32-21)28(30)31/h5-10,19H,2-4,11-17H2,1H3,(H,25,29)
  • Key:PPUYOYQTTWJTIU-UHFFFAOYSA-N

See also

References
  1. 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): 62–8. Bibcode:2012Natur.485...62S. doi:10.1038/nature11030. PMC 3343186. PMID 22460951.
  2. Banerjee S, Wang Y, Solt LA, Griffett K, Kazantzis M, Amador A, et al. (December 2014). "Pharmacological targeting of the mammalian clock regulates sleep architecture and emotional behaviour". Nature Communications. 5: 5759. Bibcode:2014NatCo...5.5759B. doi:10.1038/ncomms6759. PMC 4495958. PMID 25536025.
  3. Ercolani L, Ferrari A, De Mei C, Parodi C, Wade M, Grimaldi B (October 2015). "Circadian clock: Time for novel anticancer strategies?". Pharmacological Research. 100: 288–95. doi:10.1016/j.phrs.2015.08.008. PMID 26319800.
  4. Thevis M, Schänzer W (March 2016). "Emerging drugs affecting skeletal muscle function and mitochondrial biogenesis - Potential implications for sports drug testing programs". Rapid Communications in Mass Spectrometry. 30 (5): 635–51. Bibcode:2016RCMS...30..635T. doi:10.1002/rcm.7470. PMID 26842585.
  5. Sulli G, Rommel A, Wang X, Kolar MJ, Puca F, Saghatelian A, et al. (January 2018). "Pharmacological activation of REV-ERBs is lethal in cancer and oncogene-induced senescence". Nature. 553 (7688): 351–355. Bibcode:2018Natur.553..351S. doi:10.1038/nature25170. PMC 5924733. PMID 29320480.
  6. Amador A, Kamenecka TM, Solt LA, Burris TP (April 2018). "REV-ERBβ is required to maintain normal wakefulness and the wake-inducing effect of dual REV-ERB agonist SR9009". Biochemical Pharmacology. 150: 1–8. doi:10.1016/j.bcp.2018.01.009. PMID 29355503. S2CID 205971979.
  7. Wolff SE, Wang XL, Jiao H, Sun J, Kalsbeek A, Yi CX, Gao Y (2020). "The Effect of Rev-erbα Agonist SR9011 on the Immune Response and Cell Metabolism of Microglia". Frontiers in Immunology. 11: 550145. doi:10.3389/fimmu.2020.550145. PMC 7546349. PMID 33101272.


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