NLRP3 Inhibitor, MCC950 – CAS 256373-96-3 – Calbiochem

Descrição detalhada : 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 µM) & hERG (IC50 >30 µM)., 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 µM) & hERG (IC50 >30 µM).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.
Sinónimos : NLRP3 Inhibitor, MCC950 - CAS 256373-96-3 - Calbiochem; N-(1,2,3,5,6,7-Hexahydro- s-indacen-4-ylcarbamoyl)-4-(2-hydroxy-2-propanyl)-2-furansulfonamide, Sodium, MCC-950, MCC950, Cytokine Release Inhibitory Drug 3, CRID 3, CP-456,773
Fórmula molecula r: C20H23N2O5S · Na
Armazenamento : -20C
Embalagem : 1X1EA