NAMPT activator-3, a NAT derivative, is a NAMPT activator with an EC 50 of 2.6 μM and a K D of 132 nM. NAMPT activator-3 effectively protects cultured cells from FK866 -mediated toxicity. NAMPT activator-3 exhibits strong neuroprotective efficacy in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model without any overt toxicity.