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MCC950 sodium

MCC950 sodium

产品编号 T6887   CAS 256373-96-3
别名: CRID3 sodium salt, CP-456773, CP-456773 sodium, MCC950

MCC950 sodium (CP-456773 sodium) 是一种炎症小体 NLRP3 的抑制剂 (IC50=7.5 nM in BMDMs; IC50=8.1 nM in HMDMs),具有高效选择性。MCC950 sodium 对其他炎症小体,如 AIM2、 NLRC4 或 NLRP1 没有作用。

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MCC950 sodium Chemical Structure
MCC950 sodium, CAS 256373-96-3
规格 价格/CNY 货期 数量
2 mg ¥ 297 现货
5 mg ¥ 483 现货
10 mg ¥ 728 现货
25 mg ¥ 1,520 现货
50 mg ¥ 2,660 现货
100 mg ¥ 3,180 现货
200 mg ¥ 4,650 现货
500 mg ¥ 7,360 现货
1 g ¥ 9,920 现货
1 mL * 10 mM (in DMSO) ¥ 547 现货
其他形式的 MCC950 sodium:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: MCC950 sodium (T6887)
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参考文献
产品描述 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.
靶点活性 NLRP3:7.5nM
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]
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.
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].
动物实验 C57BL/6 mice were injected intraperitoneally with 50 mg/kg MCC950.
别名 CRID3 sodium salt, CP-456773, CP-456773 sodium, MCC950
分子量 426.46
分子式 C20H23N2O5S·Na
CAS No. 256373-96-3

存储

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

溶解度

H2O: 42.7 mg/mL (100 mM)

DMSO: 42.7 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.3449 mL 11.7244 mL 23.4489 mL 58.6221 mL
5 mM 0.469 mL 2.3449 mL 4.6898 mL 11.7244 mL
10 mM 0.2345 mL 1.1724 mL 2.3449 mL 5.8622 mL
20 mM 0.1172 mL 0.5862 mL 1.1724 mL 2.9311 mL
50 mM 0.0469 mL 0.2345 mL 0.469 mL 1.1724 mL
100 mM 0.0234 mL 0.1172 mL 0.2345 mL 0.5862 mL

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TargetMol Library Books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. Grant AJ, et al. Selective NLRP3 Inflammasome Inhibitor MCC950 Suppresses Inflammation and Facilitates Healing in Vascular Materials. Adv Sci (Weinh). 2023 Jul;10(20):e2300521. 3. Jiao J, et al. MCC950, a Selective Inhibitor of NLRP3 Inflammasome, Reduces the Inflammatory Response and Improves Neurological Outcomes in Mice Model of Spinal Cord Injury. Front Mol Biosci. 2020 Mar 3;7:37.

TargetMol Library Books文献引用

1. Luo F, Lin J.Effects of Propofol Anesthesia on Pyroptosis and the Nod-Like Receptor Protein 3/Caspase-1 Pathway in the Neonatal Rat Hippocampus.Indian Journal of Pharmaceutical Sciences.2023, 85(2): 338-343. 2. Wu X, Yi X, Zhao B, et al.The volume regulated anion channel VRAC regulates NLRP3 inflammasome by modulating itaconate efflux and mitochondria function.Pharmacological Research.2023: 107016.
NLRP3-IN-16 YQ128 NLRP3-IN-21 Ruscogenin CORM-3 JC2-11 Nodinitib-1 INF39

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 高选择性抑制剂库 HIF-1化合物库 细胞焦亡化合物库 非甾体类抗炎化合物库 已知活性化合物库 NO PAINS 化合物库 抗抑郁症化合物库 表型筛选靶点鉴定库 经典已知活性库

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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。

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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 sodium 256373-96-3 Immunology/Inflammation NF-Κb NOD-like Receptor (NLR) NOD MCC 950 MCC-950 sodium inhibit CP456773 Inhibitor CRID3 sodium salt CRID3 CP-456773 CP-456773 sodium CP 456773 MCC-950 CRID 3 CRID3 sodium MCC950 CRID-3 inhibitor

 

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