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

品牌
Sigma-Aldrich
CAS
256373-96-3
货号
5.38120
规格纯度
A cell-potent, bioavailable NLRP3 inflammasome activation inhibitor. Effectively blocks caspase-1 &-11 activation, IL-1β processing and IL-1β &IL-6 secretion.
价格
1599.66 *本价格含增值税费
促销
服务
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数量
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半岛bd体育手机客户端 名称:
256373-96-3
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
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

一般描述

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-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 ?M) & hERG (IC50>30 ?M).
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-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 ?M) & hERG (IC50>30 ?M).

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.

生化/生理作用

Cell permeable: yes
Primary Target
NLRP3
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

外形

Supplied as a sodium salt.

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

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.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式 C20H23N2O5S · Na
分子量 426.46

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥97% (HPLC)
形式 powder
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
desiccated (hygroscopic)
protect from light
颜色 white
溶解性 water: 1 mg/mL
DMSO: 50 mg/mL
储存温度 ?20℃

安全信息

储存分类代码 11 - Combustible Solids
WGK WGK 3
闪点(F) Not applicable
闪点(C) Not applicable

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