IP7e is a brain-penetrant activator of nuclear receptor related protein 1 (Nurr1/NR4A2) signaling (EC50 = 3.9 nM in a reporter assay).1 In vivo, IP7e (10 mg/kg) prevents spinal cord axonal loss and demyelination and decreases spinal cord macrophage and T cell infiltration in a mouse model of experimental autoimmune encephalomyelitis (EAE).2
|1. Hintermann, S., Chiesi, M., von Krosigk, U., et al. Identification of a series of highly potent activators of the Nurr1 signaling pathway. Bioorg. Med. Chem. Lett. 17(1), 193-196 (2007).|2. Montarolo, F., Raffaele, C., Perga, S., et al. Effects of isoxazolo-pyridinone 7e, a potent activator of the Nurr1 signaling pathway, on experimental autoimmune encephalomyelitis in mice. PLoS One 9(9), e108791 (2014).