产品描述:
RIPA-56 is an inhibitor of receptor interacting serine/threonine kinase 1 (RIPK1; IC50 = 13 nM).{60328} It is selective for RIPK1 over RIPK3 at 10 µM, as well as over a panel of additional kinases at 2 µM. RIPA-56 inhibits Z-VAD-FMK-induced necrosis in HT-29 cells (EC50 = 28 nM). In vivo, RIPA-56 (6 mg/kg) reduces TNF-α-induced lethality and protects against TNF-α-induced organ damage in a mouse model of systemic inflammatory response syndrome (SIRS). It reduces spinal cord demyelination and breakdown of the blood-brain barrier (BBB) in a mouse model of experimental autoimmune encephalomyelitis (EAE).{60329} RIPA-56 (300 mg/kg) reduces hepatic inflammatory cell infiltration and fibrosis, as well as body weight gain and total fat mass, in a mouse model of high-fat diet-induced non-alcoholic steatohepatitis (NASH).{60330}