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MCC950

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产品编号 T3701Cas号 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)。

MCC950

MCC950

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纯度: 97%
产品编号 T3701 别名 CP-456773Cas号 210826-40-7

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)。

规格价格库存数量
2 mg
¥ 369
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5 mg
¥ 498
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10 mg
¥ 790
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25 mg
¥ 1,620
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50 mg
¥ 2,656
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100 mg
¥ 3,580
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1 mL x 10 mM (in DMSO)
¥ 550
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产品介绍

生物活性
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
BMDM:7.5nM, HMDM:8.1 nM
体外活性
MCC950以纳摩尔浓度阻断NLRP3的典型与非典型激活,特异性地抑制NLRP3而不影响AIM2、NLRC4或NLRP1的激活。在小鼠骨髓来源的巨噬细胞(BMDM)和人源单核细胞衍生的巨噬细胞(HMDM)中测试了MCC950对NLRP3炎症体激活的影响,BMDM中MCC950的半抑制浓度(IC50)约为7.5 nM,而在HMDM中具有相似的抑制能力(IC50=8.1 nM)。MCC950还呈剂量依赖性地抑制IL-1β的分泌,但不抑制TNF-α的分泌。在非典型途径激活下,MCC950特异性阻断由caspase-11直接引起的NLRP3激活和IL-1β的分泌。即使在10 μM的浓度下,MCC950也不抑制由沙门氏菌(Salmonella typhimurium)激活的NLRC4刺激的IL-1β和TNF-α的分泌。在响应S. typhimurium时,MCC950不抑制caspase-1的激活或IL-1β的处理。MCC950处理对细胞裂解物中的pro-caspase-1和pro-IL-1β的表达没有显著影响[1]。
体内活性
MCC950通过减少白介素-1β (IL-1β) 的产生和减轻实验性自身免疫性脑炎症(EAE) 的严重程度,来延缓多发性硬化症模型的发展。MCC950预处理能降低IL-1β和IL-6的血清浓度,但对TNF-α的数量影响不大。在小鼠身上应用MCC950能延缓EAE的发病时间并减轻症状。通过对第22天牺牲小鼠的脑部单核细胞进行细胞内细胞因子染色和流式细胞术(FACS)分析显示,与PBS处理的小鼠相比,MCC950处理的小鼠中IL-17和IFN-γ产生的CD3+ T细胞的频率有轻微降低。具体来说,IFN-γ和特别是IL-17产生的细胞数量在CD3+ T细胞的CD4+和γδ+亚群中也有所减少。
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
化学信息
分子量404.48
分子式C20H24N2O5S
CAS No.210826-40-7
SmilesCC(C)(O)c1coc(c1)S(=O)(=O)NC(=O)Nc1c2CCCc2cc2CCCc12
密度1.396 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 83.33 mg/mL (206.02 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.4723 mL12.3616 mL24.7231 mL123.6155 mL
5 mM0.4945 mL2.4723 mL4.9446 mL24.7231 mL
10 mM0.2472 mL1.2362 mL2.4723 mL12.3616 mL
20 mM0.1236 mL0.6181 mL1.2362 mL6.1808 mL
50 mM0.0494 mL0.2472 mL0.4945 mL2.4723 mL
100 mM0.0247 mL0.1236 mL0.2472 mL1.2362 mL

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计算器

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  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 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。
% DMSO
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