Synthesis of a novel human PPARdelta selective agonist and its stimulatory effect on oligodendrocyte differentiation.
Article Details
- CitationCopy to clipboard
Sakuma S, Endo T, Kanda T, Nakamura H, Yamasaki S, Yamakawa T
Synthesis of a novel human PPARdelta selective agonist and its stimulatory effect on oligodendrocyte differentiation.
Bioorg Med Chem Lett. 2011 Jan 1;21(1):240-4. doi: 10.1016/j.bmcl.2010.11.030. Epub 2010 Nov 11.
- PubMed ID
- 21112784 [ View in PubMed]
- Abstract
We successfully synthesized a novel peroxisome proliferator-activated receptor (PPAR)delta selective agonist, namely, compound 20, with a characteristic benzisoxazole ring. Compound 20 exhibited potent human PPARdelta transactivation activity and high delta selectivity. Further, it stimulated differentiation of primary oligodendrocyte precursor cells in vitro, indicating that it may be an effective drug in the treatment of demyelinating disorders such as multiple sclerosis.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Cardarine Peroxisome proliferator-activated receptor alpha EC 50 (nM) 990 N/A N/A Details Cardarine Peroxisome proliferator-activated receptor delta EC 50 (nM) 1.7 N/A N/A Details GW-590735 Peroxisome proliferator-activated receptor alpha EC 50 (nM) 10 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor alpha EC 50 (nM) >10000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor delta EC 50 (nM) >10000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 100 N/A N/A Details