Chemistry:CGP 52608

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CGP 52608
CGP 52608.svg
Names
IUPAC name
3-Methyl-1-[(4-oxo-3-prop-2-enyl-1,3-thiazolidin-2-ylidene)amino]thiourea
Identifiers
3D model (JSmol)
ChemSpider
UNII
Properties
C8H12N4OS2
Molar mass 244.33 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references
Tracking categories (test):

CGP 52608 is a selective ligand of the RAR-related orphan receptor alpha.[1] It has been used as a biochemical tool to investigate nuclear and membrane signaling of melatonin.[1] CGP 52608 has also been reported to possess antiarthritic activity.[2] The pharmaceutical company Novartis brought it to clinical trials for rheumatoid arthritis, but development was discontinued in 2006.[3]

CGP 52608 contains a thiazolinidinedione group.[4]

References

  1. 1.0 1.1 "Transcriptional activation of the nuclear receptor RZR alpha by the pineal gland hormone melatonin and identification of CGP 52608 as a synthetic ligand". Nucleic Acids Res. 23 (3): 327–33. February 1995. doi:10.1093/nar/23.3.327. PMID 7885826. 
  2. "Thiazolidine diones, specific ligands of the nuclear receptor retinoid Z receptor/retinoid acid receptor-related orphan receptor alpha with potent antiarthritic activity". J. Biol. Chem. 271 (23): 13515–22. June 1996. doi:10.1074/jbc.271.23.13515. PMID 8662835. 
  3. "CGP 52608". Adis Insight. https://adisinsight.springer.com/drugs/800007754. 
  4. Winczyk, K; Pawlikowski, M; Karasek, M (Sep 2001). "Melatonin and RZR/ROR receptor ligand CGP 52608 induce apoptosis in the murine colonic cancer". J Pineal Res 31 (2): 179–82. doi:10.1034/j.1600-079x.2001.310213.x. PMID 11555175. 

External links