Necrostatin-1

Necrostatin-1 (Nec-1) is a potent and cross the blood-brain barrier necroptosis inhibitor with an EC₅₀ of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC₅₀=182 nM). Necrostatin-1 is also an IDO inhibitor^[1]. IC50 & Target: EC50: 182 nM (RIP1 kinase)^[1] In Vitro: Necrostatin-1 (Nec-1) efficiently inhibits the TNFα-induced necrotic death of L929 cells, which does not require exogenous caspase inhibitors^[1].
Necrostatin-1 (Nec-1) prevents radiocontrast media (RCM)-induced dilation of peritubular capillaries, suggesting a novel role unrelated to cell death for the RIP1 kinase domain in the regulation of microvascular hemodynamics and pathophysiology of contrast-induced AKI (CIAKI)^[2].
Necrostatin-1 (Nec-1) (30 µM) increases the survival of cardiomyocyte progenitor cell (CMPCs) by inhibiting necrotic cell death^[4]. In Vivo: Necrostatin-1 (Nec-1) induces tubular bilation and affects the kinetics of the dilation of peritubular capillaries after RCM application. Upon a single intraperitoneal application of a single dose of Necrostatin-1 (1.65 mg/kg body weight, i.p.) 15 minutes before RCM, the return to baseline levels is prevented within the observation period^[2].