1. Immunology/Inflammation
  2. NOD-like Receptor (NLR)
  3. MCC950

MCC950  (Synonyms: CP-456773; CRID3)

目录号: HY-12815 纯度: 99.41%
COA 产品使用指南

MCC950 (CP-456773; CRID3) 是一种有效,选择性的 NLRP3 抑制剂,在 BMDMs 和 HMDMs中的 IC50 分别为 7.5 nM 和 8.1 nM。

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MCC950 Chemical Structure

MCC950 Chemical Structure

CAS No. : 210826-40-7

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥660
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5 mg ¥600
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10 mg ¥950
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25 mg ¥1950
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50 mg ¥3200
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100 mg ¥5000
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200 mg   询价  
500 mg   询价  

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 239 篇科研文献

WB
IF

    MCC950 purchased from MCE. Usage Cited in: J Agric Food Chem. 2023 May 4.  [Abstract]

    MCC950 (10 μM; 2 h) markedly inhibits the expressionof NLRP3, Cleaved Caspase-1, and Cleaved IL-1β in HUVECs.

    MCC950 purchased from MCE. Usage Cited in: Int J Mol Sci. 2023 Mar 27.

    MCC950 (5 μM; every other day for four weeks) significantly decreases CD68+ and GSDMD+ cells in rats.

    MCC950 purchased from MCE. Usage Cited in: Journal of Traditional and Complementary Medicine. 2023 Mar 29.

    MCC950 (10 μM; 1 h) inhibits the expression of NLRP3 in THP-1 cells.

    MCC950 purchased from MCE. Usage Cited in: EMBO J. 2022 Oct 17;e111173.  [Abstract]

    BMDMs isolated from Phb1F/F mice and Phb1MyeKO mice are incubated with MCC950 (50 nM) for 30 min and are subsequently stimulated by LPS (200 ng/ml) for 6 h and ATP (4 mM) for 45 min. Protein levels in whole cell lysates and culture medium are detected by WB assay.

    MCC950 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Mar 24;15(1):95.  [Abstract]

    Chronic PVN infusion of MCC950 significantly decreases apoptosis-associated speck-like protein (ASC), pro-caspase-1, and IL-1β expression in high-salt diet rats.

    MCC950 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Sep 20;9(10):946.   [Abstract]

    The efficiency of MCC950, and its effect on caspase-1 activation and IL-1β production in As2O3-treated HepG2 cells.

    MCC950 purchased from MCE. Usage Cited in: Neurobiol Dis. 2018 Sep;117:15-27.  [Abstract]

    Effect of MCC950 on the expression of NLRP3 inflammasome components and substrates after traumatic brain injury (TBI).

    MCC950 purchased from MCE. Usage Cited in: Biofactors. 2018 Mar;44(2):123-136.  [Abstract]

    NLRP3, Casp1 p20, IL-1b, and ICAM-1 protein levels are assessed in the cell lysates by Western blotting.

    MCC950 purchased from MCE. Usage Cited in: Clin Exp Immunol. 2018 Nov;194(2):231-243.  [Abstract]

    MCC950 treatment inhibits Nucleotide-binding, oligomerization domain (NOD)-like receptor family, pyrin domain containing 3 (NLRP3) inflammasome pathway activation.

    MCC950 purchased from MCE. Usage Cited in: Molecules. 2018 Feb 27;23(3). pii: E522.  [Abstract]

    Effects of MCC950 on hippocampal NLRP3 inflammasome activation in db/db mice. Western blot analysis of NLRP3 inflammasome-associated NLRP3, ASC, IL-1β, and β-actin are performed in the hippocampus of each group.

    MCC950 purchased from MCE. Usage Cited in: Dig Dis Sci. 2018 Jan;63(1):81-91.  [Abstract]

    The expression of various molecules in pyroptotic and apoptotic pathways is detected by western blot. Representative bands from densitometric analysis in experimental groups are presented. M, MCC950 group (an inhibitor of NLRP3).

    MCC950 purchased from MCE. Usage Cited in: J Am Heart Assoc. 2017 Sep 4;6(9). pii: e006347.  [Abstract]

    Cells are pretreated with YVAD(10 μM) or MCC950 (10 μM) for 2 hours, and then exposed to TMAO (600 μM) for a further 24 hours. Expression of IL-1β, ICAM-1, MMP-9, and caspase-1 p20 is detected via Western blot.

    MCC950 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2017 Oct 3;1864(1):1-10.  [Abstract]

    MCC950 or vehicle control (PBS) is administered at 1, 4 and 6 day after Ang II infusion in the absence or presence of EMD638683. Representative images and quantification of picrosirius red-stained collagen in the heart at 7 days after Ang II infusion.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    MCC950 (CP-456773; CRID3) is a potent and selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.

    IC50 & Target

    NLRP3

     

    体外研究
    (In Vitro)

    MCC950 blocks canonical and non-canonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibits NLRP3 but not AIM2, NLRC4 or NLRP1 activation. The effect of MCC950 on NLRP3 inflammasome activation is tested in mouse bone marrow derived macrophages (BMDM) and human monocyte derived macrophages (HMDM). The IC50 of MCC950 in BMDM is approximately 7.5 nM, while in HMDM it has a similar inhibitory capacity (IC50=8.1 nM). MCC950 also dose dependently inhibit IL-1β but not TNF-α secretion.MCC950 specifically blocks caspase-11-directed NLRP3 activation and IL-1β secretion upon stimulation of the non-canonical pathway. NLRC4-stimulated IL-1β and TNF-α secretion (as activated by Salmonella typhimurium) are not inhibited by MCC950 even at a concentration of 10 µM. MCC950 does not inhibit caspase-1 activation or IL-1β processing in response to S. typhimurium. The expression of pro-caspase-1 and pro-IL-1β in cell lysates is not substantially affected by MCC950 treatment[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    MCC950 reduces Interleukin-1p (IL-1β) production and attenuates the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis. Pre-treatment with MCC950 reduces serum concentrations of IL-1β and IL-6 while it does not considerably decrease the amount of TNF-α. Treatment of mice with MCC950 delays the onset and reduced the severity of EAE. Intracellular cytokine staining and FACS analysis of brain mononuclear cells from mice sacrificed on day 22 shows modestly reduced frequencies of IL-17 and IFN-γ producing CD3+ T cells in MCC950 treated mice in comparison with PBS-treated mice. IFN-γ and particularly IL-17 producing cell numbers are also reduced in both the CD4+ and γδ+ sub-populations of CD3+ T cells[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    404.48

    Formula

    C20H24N2O5S

    CAS 号
    性状

    固体

    颜色

    White to light yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    H2O 中的溶解度 : 31.25 mg/mL (77.26 mM; ultrasonic and adjust pH to 10 with NaOH)

    DMSO 中的溶解度 : ≥ 28 mg/mL (69.22 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4723 mL 12.3616 mL 24.7231 mL
    5 mM 0.4945 mL 2.4723 mL 4.9446 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.18 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.18 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.43%

    参考文献
    Cell Assay
    [1]

    BMDM are seeded at 5×105/mL or 1×106/mL, HMDM at 5×105/mL and PBMC at 2×106/mL or 5×106/mL in 96 well plates. The following day the overnight medium is replaced and cells are stimulated with 10 ng/mL LPS from Escherichia coli serotype EH100 (ra) TLRgrad for 3 h. Medium is removed and replaced with serum free medium (SFM) containing DMSO (1:1,000), MCC950 (0.001-10 µM), Parthenolide (10 µM) or Bayer cysteinyl leukotriene receptor antagonist 1-(5-carboxy-2{3-[4-(3-cyclohexylpropoxy)phenyl]propoxy}benzoyl)piperidine-4-carboxylic acid (40 µM) for 30 min. Cells are then stimulated with inflammasome activators: 5 mM adenosine 5’-triphosphate disodium salt hydrate (ATP) (1 h), 1 µg/mL Poly(deoxyadenylic-thymidylic) acid sodium salt (Poly dA:dT) transfected with Lipofectamine 200 (3-4 h), 200 µg/mL MSU (overnight) and 10 µM nigericin (1 h) or S. typhimurium UK-1 strain. Cells are also stimulated with 25 µg/mL Polyadenylic-polyuridylic acid (4 h). For non-canonical inflammasome activation cells are primed with 100 ng/mL Pam3CSK4 for 4 h, medium is removed and replaced with SFM containing DMSO or MCC950 and 2 µg/mL LPS is transfected using 0.25% FuGENE for 16 h. Supernatants are removed and analysed using ELISA kits. LDH release is measured using the CytoTox96 non-radioactive cytotoxicity assay[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice[1]
    C57BL/6 mice are immunized subcutaneously with 150 µg of MOG peptide 35-55 emulsified in CFA containing 4 mg/mL (0.4.mg/mouse) of heat-killed MTB. Mice are injected i.p. with 500 ng pertussis toxin (PT: kaketsuken) on days 0 and 2. MCC950 is administered i.p. to mice (10 mg/kg) at induction of the disease, day 0, 1 and 2 and every 2 days thereafter. Control mice are administered vehicle (PBS) at the same time points. Mice are observed for clinical signs of disease daily (unblinded). Disease severity is scored as follows: no clinical signs, 0; limp tail, 1; ataxic gait, 2; hind limb weakness, 3; hind limb paralysis, 4; and tetra paralysis, 5.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 2.4723 mL 12.3616 mL 24.7231 mL 61.8078 mL
    5 mM 0.4945 mL 2.4723 mL 4.9446 mL 12.3616 mL
    10 mM 0.2472 mL 1.2362 mL 2.4723 mL 6.1808 mL
    15 mM 0.1648 mL 0.8241 mL 1.6482 mL 4.1205 mL
    20 mM 0.1236 mL 0.6181 mL 1.2362 mL 3.0904 mL
    25 mM 0.0989 mL 0.4945 mL 0.9889 mL 2.4723 mL
    30 mM 0.0824 mL 0.4121 mL 0.8241 mL 2.0603 mL
    40 mM 0.0618 mL 0.3090 mL 0.6181 mL 1.5452 mL
    50 mM 0.0494 mL 0.2472 mL 0.4945 mL 1.2362 mL
    60 mM 0.0412 mL 0.2060 mL 0.4121 mL 1.0301 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    MCC950
    目录号:
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