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

538120
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₀H₂₃N₂O₅S·Na 256373-96-3

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      5.38120.0001
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          Glass bottle 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
          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

          Documentation

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

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          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.
          Data Sheet

          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 -20°C
          Hygroscopic
          Protect from light
          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.