SR9011

SR9011
SR9011
SR9011.svg
식별자
  • 3-((4-클로로벤질)((5-니트로티오펜-2-일)메틸)-N-펜틸피롤리딘-1-카르복사미드
CAS 번호
PubChem CID
켐스파이더
유니
첸블
화학 및 물리 데이터
공식C23H31클론N4O3S
몰 질량479.04 g/120−1
3D 모델(JSmol)
  • CCCNC(=O)N1CC(CN(Cc2cc(Cl)cc2)CC3cc(s3)[N+](=O)[O-])C1
  • InChI=1S/C23H31ClN4O3S/c1-2-3-4-12-23(29)27-13-11-19(16-27)15-26(14-18-5-20(24)8-6-18)17-21-10-22(31)
  • 키 : PPUYOYQTTWJTIU-UHFFFAOYSA-N

SR9011은 Scripps의 Thomas Burris 교수가 Rev-ErbAα의 작용제로서50 개발한 연구약으로, Rev-Erbα의 경우 IC50 = Rev-Erbaβ의 [1]경우 560nM이다.그것은 일주기 리듬의 조절과 면역 체계 기능, 염증 및 [2][3][4][5][6][7]암과의 연관성에 대한 연구에 사용되어 왔다.

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레퍼런스

  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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