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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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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      256373-96-3C₂₀H₂₃N₂O₅S·Na
      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
      HS Code2935 90 99
      Hygroscopic Hygroscopic
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetNLRP3
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      538120 0

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

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

      TitelChargennummer
      538120

      Literatur

      Übersicht
      Coll, 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.
      Datenblatt

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision25-June-2016 JSW
      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
      DescriptionA 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).
      FormWhite powder
      FormulationSupplied as a sodium salt.
      Intert gas (Yes/No) Packaged under inert gas
      CAS number256373-96-3
      Chemical formulaC₂₀H₂₃N₂O₅S·Na
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml) or H₂O (1 mg/ml)
      Storage Protect from light
      -20°C
      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.
      Toxicity Standard Handling
      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.