Background
The synthetic retinoic acid analog AM-580 displays high selectivity for nuclear retinoic acid receptors (RAR), binding RARα more potently (EC50 = 0.3 nM) than either RARβ (EC50 = 8.6 nM) or RARγ (EC50 = 13 nM) (1,2). Signaling pathways controlled by retinoic acid coordinate cell proliferation, differentiation, apoptosis, and development of many organs and tissues (3). Treatment of a mouse model of Alzheimer's Disease (AD) with the retinoid receptor agonist AM-580 produced an anti-inflammatory effect and regulated the neurotoxic activation of microglia, shifting microglial activity toward a neuroprotective phenotype (4). AM-580 also interrupts the life cycle of diverse viruses by inhibiting host lipid biosynthesis through interaction with sterol regulatory element binding protein (SREBP), which binds sterol response elements in the promoter/enhancer regions of multiple lipogenic genes (5). In a screen of multiple antiviral agents, AM-580 exhibited anti-SARS-CoV-2 activity, with AM-580 treatment producing a substantial reduction in viral load (6).
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- Charton, J. et al. (2009) Bioorg Med Chem Lett 19, 489-92.
- Ghyselinck, N.B. and Duester, G. (2019) Development 146, dev167502. doi: 10.1242/dev.167502.
- Ganz, T. et al. (2022) J Neuroinflammation 19, 5.
- Yuan, S. et al. (2019) Nat Commun 10, 120.
- Yuan, S. et al. (2020) Viruses 12, 628. doi: 10.3390/v12060628.
Molecular Formula
C22H25NO33
Molecular Weight
351.4 g/mol
Purity
>98%
CAS
102121-60-8
Solubility
Soluble in DMSO at 35 mg/mL or ethanol at 18 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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