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

538120
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Overview

Replacement Information

Key Spec Table

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

Products

Catalogue NumberPackaging Qty/Pack
5.38120.0001 Glass bottle 10 mg
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
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
Catalogue Number GTIN
5.38120.0001 04054839059308

Documentation

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

Title

Safety Data Sheet (SDS) 

NLRP3 Inhibitor, MCC950 - CAS 256373-96-3 - Calbiochem Certificates of Analysis

TitleLot Number
538120

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 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.