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CMS121 is a substituted quinoline that has neuroprotective, anti-inflammatory, antioxidative, and renoprotective activities.1,2,3 It maintains glutathione (GSH) levels in HT22 mouse hippocampal cells in vitro in the presence of glutamate, induces differentiation of PC12 cells, prevents LPS-induced N9 microglial activation by 82% in N9 microglia, and scavenges free radicals in a Trolox equivalent activity concentration (TEAC) assay.1 CMS121 protects against ischemia and oxytosis in phenotypic screens in HT22 cells in vitro with EC50 values of 7 and 200 nM for preventing iodoacetic acid- or glutamate-induced cell death, respectively.2 It is also renoprotective, decreasing kidney weight loss and decreasing the expression of TNF-α, caspase-1, and inducible nitric oxide synthase (iNOS) in a SAMP8 mouse model of chronic kidney disease associated with rapid aging when administered at a dose of 10 mg/kg per day starting at nine months of age.3
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1. Chemical modification of the multi-
2. Back to the future with phenotypic screening. ACS Chem Neurosci. 5(7), 503-513 (2014).
3. Prevention and treatment of aging and neurodegenerative diseases. (2017).