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- CAS号：
256373-96-3
- 规格：
1g/1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg/200mg/500mg
| 规格： | 1g | 产品价格： | ￥7936.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥437.0 |
| 规格： | 2mg | 产品价格： | ￥253.0 |
| 规格： | 5mg | 产品价格： | ￥386.0 |
| 规格： | 10mg | 产品价格： | ￥582.0 |
| 规格： | 25mg | 产品价格： | ￥1216.0 |
| 规格： | 50mg | 产品价格： | ￥2128.0 |
| 规格： | 100mg | 产品价格： | ￥2544.0 |
| 规格： | 200mg | 产品价格： | ￥3720.0 |
| 规格： | 500mg | 产品价格： | ￥5888.0 |
Product Introduction
Bioactivity
| 名称 | MCC950 sodium |
| 描述 | MCC950 sodium (CP-456773 sodium) is a potent and selective inhibitor of the inflammatory vesicle NLRP3 (IC50=7.5 nM in BMDMs; IC50=8.1 nM in HMDMs). MCC950 sodium has no effect on other inflammatory vesicles such as AIM2, NLRC4 or NLRP1. |
| 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 | kinase activity assays: All assays are carried out in 384-well white microtiter plates. Compounds are 4-fold serially diluted in 8 steps, starting from 10 μM. The reaction mixture consisted of 25 μL assay buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 5 mM MnCl2, 1 mM DTT, 0.1 mM Na3VO4, 5 mM β-glycerol phosphate). For FLT3 assays, the reaction contains 2.0 μg/mL FLT3 enzyme, 5 μM of poly(Glu,Tyr) substrate and 4 μM of ATP. For JAK1 assays, the reaction contains 2.5 μg/mL of JAK1 enzyme, 10 μM of poly(Glu,Ala,Tyr) substrate and 1.0 μM of ATP. For JAK2 assays, the reaction contained 0.35 μg/mL of JAK2 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 0.15 μM of ATP. For JAK3 assays, the reaction contained 3.5 μg/mL of JAK3 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 6.0 μM of ATP. For TYK2 assays, the reaction contained 2.5 μg/mL of TYK2 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 0.15 μM of ATP. The reaction is incubated at room temperature for 2 h prior to addition of 13 μL PKLight? detection reagent. After 10 min incubation luminescent signals are read on a multi-label plate reader. |
| 动物实验 | C57BL/6 mice were injected intraperitoneally with 50 mg/kg MCC950. |
| 体外活性 | 方法：小鼠骨髓衍生的巨噬细胞 BMDM 用 LPS (10 ng/mL) 刺激 3 h，用 MCC950 sodium (1-1000 nM) 刺激 30 min，再用 ATP (5 mM) 处理 1 h，使用 ELISA 方法检测 IL-1β 和 TNF-α 水平。 结果：MCC950 处理细胞可剂量依赖性地抑制 BMDM 中 IL-1β 的释放。LPS 依赖性 TNF-α 分泌未被 MCC950 损害。[1] 方法：小鼠巨噬细胞、人冠状动脉内皮细胞和平滑肌细胞用 MCC950 sodium (0.02-20 μM) 处理 3 天，使用 Alamar Blue assay 检测细胞活力。 结果：MCC950 sodium 对三种细胞无毒性作用。[2] |
| 体内活性 | 方法：为检测体内抗 NLRP3 活性，将 MCC950 sodium (20 mg/kg) 腹腔注射给人 CAPS 疾病 MWS 的小鼠模型，每天一次，持续四周。 结果：MCC950 拯救 CAPS 小鼠模型并抑制人 MWS 细胞中的 NLRP3。[1] 方法：为研究对体内实验性脊髓损伤模型和体外神经元损伤的药理作用，将 MCC950 sodium (10-50 mg/kg) 腹腔注射给脊髓损伤 (SCI) 的 C57BL/6 小鼠。 结果：MCC950 改善了 SCI 小鼠的握力、后肢运动、脊髓水肿和病理损伤。它通过阻断 NLRP3 炎症小体组装以及促炎细胞因子 TNF-α、IL-1β 和 IL-18 的释放来发挥这种作用。[3] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : 42.7 mg/mL (100.13 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (11.72 mM), Sonication is recommended. DMSO : 250 mg/mL (586.22 mM), Sonication is recommended. |
| 关键字 | NODlikeReceptor(NLR) | NODlikeReceptor | NOD-like Receptor (NLR) | NODlike Receptor (NLR) | NOD-like Receptor | NLRP3 | NLR | MCC-950 sodium | MCC950 sodium | MCC-950 | MCC 950 | CRID3 sodium | 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 | Stavudine | N4-Acetylcytidine | Ascorbyl palmitate | MCC950 | Diisononyl phthalate |
| 相关库 | Inhibitor Library | Anti-Breast Cancer Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Anti-Alzheimer's Disease Compound Library | Highly Selective Inhibitor Library | Anti-Aging Compound Library | Anti-Ovarian Cancer Compound Library | Anti-Liver Cancer Compound Library | Nonsteroidal Anti-Inflammatory Compound Library | Antioxidant Compound Library | Immunology/Inflammation Compound Library |
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相关实验
DNA Methylation Analysis by Bisulfite Sequencing (BS)
DNA plays a key role in the regulation of gene expression. There is an extensive range of methods based on the sodium bisulfite treatment for quantifying the methylation status of cytosines located in specific DNA regions. Bisulfite modification
⑴无机化合物的特点 ①无机化合物和溴化钾、氯化钠之间会发生离子交换作用。因此无机化合物样品制备和有机化合物不同。用溴化钾压片或直接涂于氯化钠盐片上都不合适，最好用石蜡油法。 ②由单原子构成的离子型固体，如氯化钠，溴化钾等，仅用单陈振动，多出现在300cm-1左右，但多离子化合物却在600~4000 cm-1区有吸收带。无机分析一般还是看它的阴离子。如碳酸根在1450~1410 cm-1及880~800 cm-1；磷酸根则在1100~950 cm-1;硫酸
⑴无机化合物的特点 ①无机化合物和溴化钾、氯化钠之间会发生离子交换作用。因此无机化合物样品制备和有机化合物不同。用溴化钾压片或直接涂于氯化钠盐片上都不合适，最好用石蜡油法。 ②由单原子构成的离子型固体，如氯化钠，溴化钾等，仅用单陈振动，多出现在300cm-1左右，但多离子化合物却在600~4000 cm-1区有吸收带。无机分析一般还是看它的阴离子。如碳酸根在1450~1410 cm-1及880~800 cm-1；磷酸根则在1100~950 cm-1;硫酸根在1110
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化合物 MCC950 sodium【256373-96-3】
￥253 - 7936
