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Beschreibung

A cell-permeable, bioavailable, non-toxic sulfonylurea derived compound that selectively interacts with NLRP3 inflammasome and prevents its activation in a reversible manner with no effect on NLRC4 and NLRP1. Dose-dependently reduces IL-1beta production (IC50 = 7.5 & 8.1 nM in LPS & ATP-treated BMDMs & HMDMs, respectively) with minimal effect on IL-1alpha & TNF-alpha. Specifically blocks NLRP3-dependent pyroptotic cell death by inhibiting caspase-1 &-11 activation, IL-1beta processing and ASC oligomerization. Does neither block K+ efflux, Ca2+ flux or NLRP3-ASC interactions nor inhibit NLRC4, AIM2, TLR signaling or NLRP3 priming. Effectively suppresses T cell responses and IL-1beta & IL-6 secretion, and reduces the severity of EAE and rescues neonatal lethality in a mouse model of CAPS (10 mg/kg, i.p., q.d. & 20 mg/kg, i.p., every other day, respectively). Displays attractive PK profile with desirable microsomal stability and minimal liability towards CYP450 isozymes (<15% inhibition at 10 µ,M) & hERG (IC50 >30 µ,M)., A cell-permeable, bioavailable, non-toxic sulfonylurea derived compound that selectively interacts with NLRP3 inflammasome and prevents its activation in a reversible manner with no effect on NLRC4 and NLRP1. Dose-dependently reduces IL-1beta production (IC50 = 7.5 & 8.1 nM in LPS & ATP-treated BMDMs & HMDMs, respectively) with minimal effect on IL-1alpha & TNF-alpha. Specifically blocks NLRP3-dependent pyroptotic cell death by inhibiting caspase-1 &-11 activation, IL-1beta processing and ASC oligomerization. Does neither block K+ efflux, Ca2+ flux or NLRP3-ASC interactions nor inhibit NLRC4, AIM2, TLR signaling or NLRP3 priming. Effectively suppresses T cell responses and IL-1beta & IL-6 secretion, and reduces the severity of EAE and rescues neonatal lethality in a mouse model of CAPS (10 mg/kg, i.p., q.d. & 20 mg/kg, i.p., every other day, respectively). Displays attractive PK profile with desirable microsomal stability and minimal liability towards CYP450 isozymes (<15% inhibition at 10 µ,M) & hERG (IC50 >30 µ,M).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.