基本信息

技术规格

物性(参考值)

基本信息

产品描述

MCC950(CP-456773)是一种有效的、选择性NLRP3抑制剂，在骨髓来源的巨噬细胞中IC50为7.5 nM。对AIM2, NLRC4或NLRP1炎症体没有作用。

靶点（IC50 & Targe）

NLRP3,7.5nM

体外研究

MCC950在骨髓来源的巨噬细胞和人类单核细胞衍生的巨噬细胞中，抑制经典和非经典NLRP3激活，IC50分别为7.5和8.1 nM。MCC950特异性抑制NLRP3的激活，不抑制AIM2, NLRC4或NLRP1这些炎症小体[1]。

体内研究

MCC950减少白介素-1β(IL-1β)的产生、减轻实验性自身免疫性脑脊髓炎的严重性。在自身炎症性疾病Cryopyrin蛋白相关周期性综合征的小鼠模型中，MCC950能够挽救其新生时期的死亡。在间接体外实验中，在来源于韦二氏综合征患者的样品具有活性[1]。

动物实验

Animal Models: C57BL/6小鼠

Formulation: DMSO/PBS

Dosages: 50 mg/kg

Administration: 腹腔注射

(Only for Reference)

参考文献

[1] Coll RC, et al. Nat Med. 2015, 21(3):248-55.

安全信息

图形或危害标志
危险说明	H302 H410
防范说明	P264 P270 P273 P301+P312 P330 P391 P501
UN号码	3077
危险分类	9
包装等级	III

产品说明

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 µM) & hERG (IC₅₀ >30 µM).
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 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.

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

产品性质

安全信息

产品说明

应用

CP-456773钠盐已用于：

• 在体内实验中研究生酮饮食的神经保护作用。
• 研究抑制 NLRP3(nod样受体蛋白3)炎性体活性对小鼠模型肿瘤进展的影响。
• 研究胆固醇晶体介导的IL-1b(白细胞介素-1b)在胎盘外植体中的反应。

包装

5, 25 mg in glass bottle

生化/生理作用

已知 CP-456773抑制其他促炎细胞因子(如IL-1α和IL-18)的释放。它也被称为MCC950。
CP-456773钠盐(CRID3)是一种细胞因子释放抑制药物，也是NLRP3 炎性体的抑制剂。CP-456773钠盐抑制白细胞介素1β(IL-1β)分泌和caspase 1 加工。

其他说明

该化合物由辉瑞开发，用于细胞因子和细胞因子 & 生长因子的研究。要了解 Sigma 与辉瑞公司合作的更多信息，并查看其他正宗的、高品质辉瑞化合物，请见sigma.com/bsm-pfizer。

法律信息

根据辉瑞公司的协议，出售用于研究目的
Pfizer is a registered trademark of Pfizer, Inc.

基本信息

产品性质

安全信息