Coumarin 478

Coumarin 478 is a synthetic coumarin and an antagonist of farnesoid X receptor (FXR) and DAF-12, the C. elegans functional ortholog.¹ It inhibits agonist-induced activation of FXR or DAF-12 in reporter assays at 30 µM. Coumarin 478 inhibits mitochondrial reactive oxygen species (ROS) production induced by rotenone (Item No. 13995) and increases the oxygen consumption rate in C2C12 cells. It induces mitophagy in C. elegans neurons and body wall muscles and increases the lifespan of C. elegans. Coumarin 478 reduces amyloid-β (1-42)-induced paralysis and α-synuclein-induced thrashing in transgenic C. elegans expressing these human neurotoxic proteins in the muscles. It also inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE; IC₅₀s = 10.7 and 27.8 µM, respectively) and is active against C. pneumoniae at 50 µM.^2,3 Coumarin 478 displays absorption/emission maxima of 386/478 nm, respectively.⁴

WARNING This product is not for human or veterinary use.

1. Fallarero, A., Oinonen, P., Gupta, S., et al. Inhibition of acetylcholinesterase by coumarins: The case of coumarin 106. Pharmacol. Res. 58(3-4), 215-221 (2008).

2. Tan, L., Shan, H., Han, C., et al. Discovery of potent OTUB1/USP8 dual inhibitors targeting proteostasis in non-small-cell lung cancer. J. Med. Chem. 65(20), 13645-13659 (2022).

3. Alvesalo, J., Vuorela, H., Tammela, P., et al. Inhibitory effect of dietary phenolic compounds on Chlamydia pneumoniae in cell cultures. Biochem. Pharmacol. 71(6), 735-741 (2006).

4. Reynolds, G.A., and Drexhage, K.H. New coumarin dyes with rigidized structure for flashlamp-pumped dye lasers. Opt. Commun. 13(3), 222-225 (1975).