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- CAS号：
210826-40-7
- 规格：
1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥377.0 |
|---|---|---|---|
| 规格： | 2mg | 产品价格： | ￥249.0 |
| 规格： | 5mg | 产品价格： | ￥341.0 |
| 规格： | 10mg | 产品价格： | ￥541.0 |
| 规格： | 25mg | 产品价格： | ￥1096.0 |
| 规格： | 50mg | 产品价格： | ￥1816.0 |
| 规格： | 100mg | 产品价格： | ￥2448.0 |
Product Introduction
Bioactivity
| 名称 | MCC950 |
| 描述 | MCC950 (CP-456773) is a NLRP3 inflammasome inhibitor (IC50=7.5-8.1 nM). MCC950 can be used to treat inflammatory diseases, inflammation-related tumors and neurodegenerative diseases. |
| 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]. |
| 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]. |
| 体外活性 | 方法：HEK293细胞、HepG2细胞用MCC950处理后使用resazurin based fluorescence assay检测细胞毒性。 结果：MCC950对HEK293细胞（CC50> 62.5 μM）、HepG2细胞（CC50> 62.5 μM）无毒。[1] 方法：人THP-1细胞用MCC950处理72小时后使用CCK-8方法检测细胞毒性。 结果：MCC950抑制THP-1细胞生长（CC50=81.35 μM）。[2] 方法：人THP-1细胞用MCC950处理72小时后使用MTT方法检测细胞毒性。 结果：MCC950抑制THP-1细胞生长（IC50=98.83 μM）。[3] |
| 体内活性 | 方法：为研究MCC950的抗炎作用，将小鼠预先用MCC950处理1小时，然后腹腔注射LPS。 结果：2小时后检测发现，MCC950可降低血清中IL-1β和IL-6的浓度，但对TNF-α的量影响不大，表明MCC950在体内具有活性。[4] 方法：为研究MCC950的抗炎作用，使用7周大的Winnie小鼠（Muc2基因突变，C57BL/6J背景），分为MCC950治疗组和对照组，每组10只。治疗组小鼠每天喂食含有40mg/kg MCC950的新鲜饲料糊，对照组喂食不含MCC950的饲料糊，实验持续21天。 结果：MCC950治疗组小鼠的DAI评分显著降低，表明其粪便稠度和粪便中血液情况得到改善。治疗组小鼠的结肠长度增加，结肠重量减轻，说明结肠炎症减轻。H&E染色结果显示，MCC950治疗组小鼠的结肠炎症特征明显改善。[5] 方法：为研究MCC950对非肥胖糖尿病的影响，将MCC950腹腔注射给11周龄的雌性非肥胖糖尿病（NOD）小鼠，每周3次，连续3周。 结果：MCC950治疗导致唾液分泌显著减少，并加剧了下颌下腺的白细胞浸润。此外，还伴随着T细胞和B细胞数量增加、Th1反应增强以及下颌下腺中水通道蛋白5表达减少。[6] |
| 存储条件 | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (8.16 mM), Sonication is recommended. DMSO : 83.33 mg/mL (206.02 mM), Sonication is recommended. |
| 关键字 | NOD-like Receptor (NLR) | NLRP3 | MCC-950 | MCC950 | MCC 950 | Inhibitor | inhibit | CRID-3 | CRID3 | CRID 3 | CP456773 | CP 456773 |
| 相关产品 | Trimethylamine N-oxide | Teneligliptin hydrobromide | Citraconic acid | NLRP3-IN-2 | (S)-(+)-Carvone | Aluminum Hydroxide | Resveratrol | Articaine hydrochloride | Stavudine | N4-Acetylcytidine | Ascorbyl palmitate | Diisononyl phthalate |
| 相关库 | Inhibitor Library | Anti-Breast Cancer Compound Library | Pyroptosis Compound Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Aging Compound Library | Anti-Ovarian Cancer Compound Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | NF-κB Signaling Compound Library | Anti-Prostate Cancer Compound Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 MCC950【210826-40-7】
￥249 - 2448
