CGP 52608
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| IUPAC name
3-Methyl-1-[(4-oxo-3-prop-2-enyl-1,3-thiazolidin-2-ylidene)amino]thiourea
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| Identifiers | |
3D model (JSmol)
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| ChemSpider | |
PubChem CID
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| UNII | |
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| 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).
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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
[edit]- ^ a b Wiesenberg I, Missbach M, Kahlen JP, Schräder M, Carlberg C (February 1995). "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. doi:10.1093/nar/23.3.327. PMC 306679. PMID 7885826.
- ^ Missbach M, Jagher B, Sigg I, Nayeri S, Carlberg C, Wiesenberg I (June 1996). "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. doi:10.1074/jbc.271.23.13515. PMID 8662835.
- ^ "CGP 52608". Adis Insight.
- ^ 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. S2CID 6461798.
External links
[edit]- CGP+52608 at the U.S. National Library of Medicine Medical Subject Headings (MeSH)