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MCC950

MCC950

产品编号 T3701   CAS 210826-40-7
别名: CP-456773

MCC950 (CP-456773) 是NLRP3的选择性抑制剂,能够作用于BMDMs(IC50:7.5 nM) 和 HMDMs(IC50:8.1 nM)。

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MCC950 Chemical Structure
MCC950, CAS 210826-40-7
规格 价格/CNY 货期 数量
2 mg ¥ 369 现货
5 mg ¥ 665 现货
10 mg ¥ 820 现货
50 mg ¥ 3,275 现货
100 mg ¥ 6,065 现货
1 mL * 10 mM (in DMSO) ¥ 730 现货
其他形式的 MCC950:
产品目录号及名称: MCC950 (T3701)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 CP-456773 (MCC950 (CP-456773) and CRID3) is an effective and specific cytokine release inhibitor and NLRP3 inflammasome inhibitor. CP-456773 inhibits IL-1β secretion and caspase 1 processing. MCC950 blocked canonical and noncanonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibited activation of NLRP3 but not the AIM2, NLRC4 or NLRP1 inflammasomes. MCC950 reduced IL-1β production in vivo and attenuated the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis.
靶点活性 BMDMs:7.5nM, HMDMs:8.1 nM
体外活性 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].
体内活性 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].
激酶实验 Disk diffusion is conducted, except that 10 μg of each antibiotic compound is used per filter. Growth in liquid medium in the presence of CHIR-090 is evaluated as follows: cells from overnight cultures are inoculated into 50 mL portions of LB broth at an A600 of 0.02 and grown with shaking at 30°C. When the A600 reaches 0.15, parallel cultures are treated with either 6 μL of 500 μg/mL CHIR-090 in DMSO or 6 μL of DMSO. To assess cumulative growth, cultures are maintained in log phase growth by 10-fold dilution into pre-warmed medium, containing the same concentrations of DMSO or DMSO/CHIR-090, whenever the A600 reaches 0.4. The minimal inhibitory concentration is defined as the lowest antibiotic concentration at which no measurable bacterial growth is observed in LB medium containing 1% DMSO (v/v), when inoculated at a starting density of A600=0.01. Cultures are incubated with shaking for 24 h at 30°C in the presence of CHIR-090. Experiments are performed in triplicate[1].
细胞实验 MCC950 is dissolved in DMSO and stored, and then diluted with appropriate media before use[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), glyburide (200 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].
别名 CP-456773
分子量 404.48
分子式 C20H24N2O5S
CAS No. 210826-40-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 28 mg/mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Coll RC, et al. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nat Med. 2015 Mar;21(3):248-55. 2. Li L H, Chen T L, Chiu H W, et al. Critical Role for the NLRP3 Inflammasome in Mediating IL-1β Production in Shigella sonnei-Infected Macrophages[J]. Frontiers in Immunology. 2020, 11: 1115. 3. Li L H, Lin J S, Chiu H W, et al. Mechanistic insight into the activation of the NLRP3 inflammasome by Neisseria gonorrhoeae in macrophages[J]. Frontiers in Immunology. 2019, 10: 1815. 4. Li S, Hui Y, Yuan J, et al. Syk-Targeted, a New 3-Arylbenzofuran Derivative EAPP-2 Blocks Airway Inflammation of Asthma–COPD Overlap in vivo and in vitro[J]. Journal of Inflammation Research. 2021, 14: 2173-2185. 5. Wu C H, Gan C H, Li L H, et al. A Synthetic Small Molecule F240B Decreases NLRP3 Inflammasome Activation by Autophagy Induction[J]. Frontiers in Immunology. 2020, 11. 6. Xie D, Ge X, Ma Y, et al. Clemastine improves hypomyelination in rats with hypoxic–ischemic brain injury by reducing microglia-derived IL-1β via P38 signaling pathway[J]. Journal of Neuroinflammation. 2020, 17(1): 1-17. 7. Chen Y Q, Wang S N, Shi Y J, et al. CRID3, a blocker of apoptosis associated speck like protein containing a card, ameliorates murine spinal cord injury by improving local immune microenvironment[J]. Journal of Neuroinflammation. 2020, 17(1): 1-18. 8. Wei Shi, Guang Xu, Xiaoyan Zhan, Yuan Gao, Zhilei Wang, Shubin Fu, Nan Qin, Xiaorong Hou, Yongqiang Ai, Chunyu Wang, Tingting He, Hongbin Liu, Yuanyuan Chen, Yan Liu, Jiabo Wang, Ming Niu, Yuming Guo, Xiaohe Xiao & Zhaofang Bai. Carnosol inhibits inflammasome activation by directly targeting HSP90 to treat inflammasome-mediated diseases. Cell death & disease. 2020 9. Zhilei Wang, Guang Xu, Yuan Gao, Xiaoyan Zhan, Nan Qin, Shubin Fu, Ruisheng Li et al. Cardamonin from a medicinal herb protects against LPS-induced septic shock by suppressing NLRP3 inflammasome [J]. Acta Pharmaceutica Sinica B. 2019 Feb 14.

文献引用

1. Shi W, Xu G, Gao Y, et al.Novel role for epalrestat: protecting against NLRP3 inflammasome-driven NASH by targeting aldose reductase.Journal of Translational Medicine.2023, 21(1): 1-17. 2. Li N, Jiang X, Zhang R, et al.Discovery of Triazinone Derivatives as Novel, Specific, and Direct NLRP3 Inflammasome Inhibitors for the Treatment of DSS-Induced Ulcerative Colitis.Journal of Medicinal Chemistry.2023 3. Cao X, Di G, Bai Y, et al.Aquaporin5 Deficiency Aggravates ROS/NLRP3 Inflammasome-Mediated Pyroptosis in the Lacrimal Glands.Investigative Ophthalmology & Visual Science.2023, 64(1): 4-4. 4. Li Q, Zhao P, Wen Y, et al.POLYDATIN AMELIORATES TRAUMATIC BRAIN INJURY–INDUCED SECONDARY BRAIN INJURY BY INHIBITING NLRP3-INDUCED NEUROINFLAMMATION ASSOCIATED WITH SOD2 ACETYLATION.Shock.2023, 59(3): 460-468. 5. Chen Y Q, Wang S N, Shi Y J, et al. CRID3, a blocker of apoptosis associated speck like protein containing a card, ameliorates murine spinal cord injury by improving local immune microenvironment. Journal of Neuroinflammation. 2020, 17(1): 1-18. 6. Li S, Hui Y, Yuan J, et al. Syk-Targeted, a New 3-Arylbenzofuran Derivative EAPP-2 Blocks Airway Inflammation of Asthma–COPD Overlap in vivo and in vitro. Journal of Inflammation Research. 2021, 14: 2173-2185. 7. Zhang H, Gao J, Fang W, et al. Role of NINJ1 in Gout Flare and Potential as a Drug Target. Journal of Inflammation Research. 2022, 15: 5611-5620. 8. Gao Y, Xu G, Ma L, et al. Icariside I specifically facilitates ATP or nigericin-induced NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Cell Communication and Signaling. 2021 Feb 11;19(1):13. doi: 10.1186/s12964-020-00647-1. 9. Yang S R, Hua K F, Yang C Y, et al. Cf‐02, a novel benzamide‐linked small molecule, blunts NF‐κB activation and NLRP3 inflammasome assembly and improves acute onset of accelerated and severe lupus nephritis in mice. The FASEB Journal. 2021, 35(8): e21785. 10. Qin N, Xu G, Wang Y, et al. Bavachin enhances NLRP3 inflammasome activation induced by ATP or nigericin and causes idiosyncratic hepatotoxicity. Frontiers of Medicine. 2021 Aug;15(4):594-607.
11. Niu L, Luo S S, Xu Y, et al. The critical role of the hippocampal NLRP3 inflammasome in social isolation-induced cognitive impairment in male mice. Neurobiology of Learning and Memory. 2020: 107301 12. Gao Y, Xu G, Ma L, et al. Icarisid I specifically facilitates ATP or nigericin-induced NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Cell Communication and Signaling. 2020 13. Wu C H, Gan C H, Li L H, et al. A Synthetic Small Molecule F240B Decreases NLRP3 Inflammasome Activation by Autophagy Induction. Frontiers in Immunology. 2020 Dec 18;11:607564. doi: 10.3389/fimmu.2020.607564. eCollection 2020. 14. Meng Z, Liu H, Zhang J, et al. Sesamin promotes apoptosis and pyroptosis via autophagy to enhance antitumour effects on murine T-cell lymphoma. Journal of Pharmacological Sciences. 2021 15. Wei Shi, Guang Xu, Xiaoyan Zhan, Yuan Gao, Zhilei Wang, Shubin Fu, Nan Qin, Xiaorong Hou, Yongqiang Ai, Chunyu Wang, Tingting He, Hongbin Liu, Yuanyuan Chen, Yan Liu, Jiabo Wang, Ming Niu, Yuming Guo, Xiaohe Xiao & Zhaofang Bai Carnosol inhibits inflammasome activation by directly targeting HSP90 to treat inflammasome-mediated diseases. Cell Death & Disease. 2020 16. Tian C, Han X, He L, et al. Transient receptor potential ankyrin 1 contributes to the ATP-elicited oxidative stress and inflammation in THP-1-derived macrophage. Molecular and Cellular Biochemistry. 2020: 1-14 17. Li L H, Chen T L, Chiu H W, et al. Critical Role for the NLRP3 Inflammasome in Mediating IL-1β Production in Shigella sonnei-Infected Macrophages. Frontiers in Immunology. 2020, 11: 1115 18. Li L H, Lin J S, Chiu H W, et al. Mechanistic insight into the activation of the NLRP3 inflammasome by Neisseria gonorrhoeae in macrophages. Frontiers in Immunology. 2019, 10: 1815 19. Wang Z, Xu G, Gao Y, et al. Cardamonin from a medicinal herb protects against LPS-induced septic shock by suppressing NLRP3 inflammasome. Acta Pharmaceutica Sinica B. 2019, 9(4): 734-744 20. Tian C, Huang R, Tang F, et al. Transient Receptor Potential Ankyrin 1 Contributes to Lysophosphatidylcholine-Induced Intracellular Calcium Regulation and THP-1-Derived Macrophage Activation. The Journal of Membrane Biology. 2019: 1-13 21. Xie D, Ge X, Ma Y, et al. Clemastine improves hypomyelination in rats with hypoxic–ischemic brain injury by reducing microglia-derived IL-1β via P38 signaling pathway. Journal of neuroinflammation. 2020, 17(1): 1-17. 22. Ni B, Pei W, Qu Y, et al. MCC950, the NLRP3 Inhibitor, Protects against Cartilage Degradation in a Mouse Model of Osteoarthritis. Oxidative Medicine and Cellular Longevity. 2021, 2021. 23. Yuan X, Chen P, Luan X, et al.NLRP3 deficiency protects against acetaminophen‑induced liver injury by inhibiting hepatocyte pyroptosis.Molecular Medicine Reports.2024, 29(4): 1-15. 24. Chiu H W, Wu C H, Lin W Y, et al.The Angiotensin II Receptor Neprilysin Inhibitor LCZ696 Inhibits the NLRP3 Inflammasome By Reducing Mitochondrial Dysfunction in Macrophages and Alleviates Dextran Sulfate Sodium-induced Colitis in a Mouse Model.Inflammation.2024: 1-22.
收起
Physalin B Procyanidin B2 Selnoflast Nigericin sodium salt NLRP3-IN-10 Asymmetric dimethylarginine JC124 6-Biopterin

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 抗前列腺癌化合物库 抗乳腺癌化合物库

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

MCC950 210826-40-7 Immunology/Inflammation NF-Κb NOD CP 456773 MCC 950 Inhibitor CRID-3 NOD-like Receptor (NLR) inhibit CP-456773 MCC-950 CRID3 CP456773 CRID 3 inhibitor

 

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