LY 278584

• CAT Number: I007814
• CAS Number: 119193-37-2
• Molecular Formula: C17H22N4O
• Molecular Weight: 298.39
• Purity: ≥95%
• Target: 5-HT3-receptor antagonist
• Solubility: Soluble in DMSO
• Storage: 0 - 4°C for short term , or -20°C for long term.
• IUPAC Name: 1-methyl-N-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)indazole-3-carboxamide
• InChI: InChI=1S/C17H22N4O/c1-20-12-7-8-13(20)10-11(9-12)18-17(22)16-14-5-3-4-6-15(14)21(2)19-16/h3-6,11-13H,7-10H2,1-2H3,(H,18,22)
• InChIKey: DDHAJFBBJWHSBR-UHFFFAOYSA-N
• SMILES: CN1C2CCC1CC(C2)NC(=O)C3=NN(C4=CC=CC=C43)C

LY 278584 (Cat.No:I007814) is a potent and selective inhibitor of the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). This enzyme is involved in the conversion of inactive cortisone to active cortisol, a stress hormone. By inhibiting 11β-HSD1, LY 278584 may have therapeutic potential in conditions such as metabolic disorders and inflammatory diseases.

Reference

1:J Pharmacol Sci. 2010;113(3):281-4. Epub 2010 Jul 1. Changes in characteristics of the specific binding of [3H]LY-278584, a 5-HT3-receptor antagonist, on differentiated NG108-15 cells.Matsushima K,Imanishi T,Asano H,Funakami Y,Wada T,Ichida S, PMID: 20606368 Abstract: We have reported previously that the concentration of intracellular Ca2+ evoked by serotonin (5-HT) was significantly augmented in differentiated NG108-15 (NG) cells treated with dibutyryl cAMP and the enhanced response occurred via 5-HT3 receptors. We investigated changes in the characteristics for specific binding of [(3)H]LY-278584 (a specific antagonist of the 5-HT3 receptor) on membranes from differentiated NG cells. The results indicated that the K(d) and B(max) values for the specific binding to differentiated NG cells were significantly smaller and larger, respectively, than those for undifferentiated NG cells. The binding was significantly inhibited by 10 nM tropisetron, a specific 5-HT3-receptor antagonist, but not by any other types of 5-HT-receptor antagonists. These results suggested that the enhanced response by 5-HT in differentiated NG cells was due to both qualitative and quantitative changes in the 5-HT3 receptor.