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J-147(EC50= 60-115nM)
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Description
J-147 is a broad spectrum neuroprotective phenyl hydrazide compound(EC50=60-115 nM) with significant neurotrophic properties related to the induction of brain-derived neurotrophic factor (BDNF).IC50 value: 60-115 nM in vitro assay [1]Target: J-147 has been shown to promotes HT22 and primary cell survival in a dose-dependent manner (EC50 value range of 0.06 ??? 0.115 ??M) when applied to cell exposed to the mitochondrial neurotoxin, iodoacetic acid (IAA), toxicity mediated by the excitatory amino acid glutamate, which causes HT22 cell death by an oxytosis mechanism. In the preclinical in vitro development assays, the EC50 value for J-147-induced cell survival is 25 nM. J-147 was metabolically unstable (highly metabolized) with only 12% of parent remaining after incubation with rat microsomes (phase 1 metabolism).
References
[1].Lapchak PA, et al. J-147 a Novel Hydrazide Lead Compound to Treat Neurodegeneration: CeeToxTMSafety and Genotoxicity Analysis. J Neurol Neurophysiol. 2013 Aug;4(3). pii: 158.