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538120 NLRP3 Inhibitor, MCC950 - CAS 256373-96-3 - Calbiochem

A cell-potent, bioavailable NLRP3 inflammasome activation inhibitor. Effectively blocks caspase-1 & -11 activation, IL-1β processing and IL-1β & IL-6 secretion.

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Synonyme: 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

Primary Target: NLRP3
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538120
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Übersicht

Key Spec Table

CAS #Empirical Formula
256373-96-3C₂₀H₂₃N₂O₅S·Na

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5381200001
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      		 Glasflasche 10 mg
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      Description
      OverviewA 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-1β production (IC50 = 7.5 & 8.1 nM in LPS & ATP-treated BMDMs & HMDMs, respectively) with minimal effect on IL-1α & TNF-α. Specifically blocks NLRP3-dependent pyroptotic cell death by inhibiting caspase-1 &-11 activation, IL-1β 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-1β & 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.
      Catalogue Number538120
      Brand Family Calbiochem®
      SynonymsN-(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
      DescriptionNLRP3 Inhibitor, MCC950
      References
      ReferencesColl, R.C., et al. 2015. Nat. Med. 21, 248.
      Coll, R.C. and O'Neill, L.A.J. 2011. PLoS ONE. 6, e29539.
      Laliberte, R.E., et al. 2003. J. Biol. Chem. 278, 16567.
      Perregaux, D.G., et al. 2001. J. Pharmacol. Exp. Ther. 299, 187.
      Product Information
      CAS number256373-96-3
      FormWhite powder
      FormulationSupplied as a sodium salt.
      Hill FormulaC₂₀H₂₃N₂O₅S·Na
      Chemical formulaC₂₀H₂₃N₂O₅S·Na
      Hygroscopic Hygroscopic
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetNLRP3
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Bestellnummer GTIN
      5381200001 04054839059308