IP7e

IP7e is a potent, brain-penetrant and orally active Nurr1 activator with an EC50 value of 3.9 nM[1].

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

EC50: 3.9 nM (Nurr1)[1]

IP7e (Isoxazolo-pyridinone 7e; 10 mg/kg; oral gavage; twice a day) preventive treatment reduces the incidence and the severity of a MS murine model, i.e. experimental autoimmune encephalomyelitis (EAE). IP7e attenuates inflammation and neurodegeneration in spinal cords of EAE mice by an NF-kB pathway-dependent process[2]. Animal Model: Female C57BL/6J mice (6-8 week-old) with experimental autoimmune encephalomyelitis (EAE)[2]. Dosage: 10 mg/kg Administration: Oral gavage; twice a day; preventive administration (before the disease onset) from 7 to 23 d.p.i. and therapeutic (after the disease onset) from 21 to 36 d.p.i. Result: Preventive administration delayed the onset and reduces the incidence and severity of EAE, and decreased neuroinflammatory and histopathological alterations in the spinal cord of treated EAE mice. On the contrary, the course of EAE was not influenced by the therapeutic administration.

[1]. Samuel Hintermann, et al. Identification of a series of highly potent activators of the Nurr1 signaling pathway. Bioorg Med Chem Lett. 2007 Jan 1;17(1):193-6.

[2]. Francesca Montarolo, et al. Effects of isoxazolo-pyridinone 7e, a potent activator of the Nurr1 signaling pathway, on experimental autoimmune encephalomyelitis in mice. PLoS One. 2014 Sep 29;9(9):e108791.