5.38120

类端粒沉默干扰体1(NLRP3)抑制剂，MCC950

• 别名: 类端粒沉默干扰体1(NLRP3)抑制剂，MCC950
• 经验公式（希尔记法）: C₂₀H₂₃N₂O₅S · Na
• CAS号: 256373-96-3
• 分子量: 426.46
• 分類程式碼代碼: 51111800
• NACRES: NA.77

属性

• 化驗: ≥97% (HPLC)
• 品質等級: 100
• 形狀: powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; desiccated (hygroscopic); protect from light
• 顏色: white
• 溶解度: water: 1 mg/mL; DMSO: 50 mg/mL
• 儲存溫度: −20°C
• InChI: 1S/C20H24N2O5S.Na/c1-20(2,24)14-10-17(27-11-14)28(25,26)22-19(23)21-18-15-7-3-5-12(15)9-13-6-4-8-16(13)18;/h9-11,24H,3-8H2,1-2H3,(H2,21,22,23);/q;+1/p-1
• InChI 密鑰: LFQQNXFKPNZRFT-UHFFFAOYSA-M

说明

一般說明

MCC950 is an antagonist ofInterleukin-1 beta (IL-1β). It interacts with both the inactive as well as active forms of NOD-like receptor protein 3 (NLRP3) and targets the Walker B motif within the NLRP3 NACHT domain. A cell-permeable, bioavailable, non-toxic sulfonylurea-derived compound that selectively interacts with the 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, it 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 inhibits NLRC4, AIM2, TLR signaling, or NLRP3 priming. Effectively suppresses T cell responses and IL-1β& IL-6 secretion, 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 an attractive PK profile with desirable microsomal stability and minimal liability towards CYP450 isozymes (<15% inhibition at 10 µM) & hERG (IC50 >30 µM). It has demonstrated effectiveness against metabolic diseases, autoimmune diseases, cardiovascular diseases, and other conditions.

應用

MCC950 has been used in:

• hemolysis-affected mice to study the involvement of the NLRP3 inflammasome in kidney function injury.
• MCC950-mediated inflammasome inhibition assays.
• testing synergistic effect of pharmacologic inhibition of NLRP3 inflammasome in combination with immune checkpoint inhibitors (ICI) immunotherapy in tumor-bearing animals.
• studying the role of NLRP3 inflammasome in the development of endothelial dysfunction in early sepsis in mice.

生化／生理作用

主要靶标
NLRP3

可逆性：是

细胞可渗透性：具有

包裝

用惰性气体包装

警告

毒性：标准处理（A）

外觀

以钠盐供应。

重構

复溶后，等分并冷冻保存（-20°C）。贮备液在-20°C下可稳定保存至多3个月。

其他說明

Pleasenote that the molecular weight for this compound is batch-specific due tovariable water content. Please refer to the vial label or the certificate ofanalysis for the batch-specific molecular weight. The molecular weight providedrepresents the baseline molecular weight without water.

法律資訊

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

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable