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网站主页 化工产品目录 生物化工 生化试剂 激动剂抑制剂 N-[[(1,2,3,5,6,7-六氢-S-引达省-4-基)氨基]羰基]-4-(1-羟基-1-甲基乙基)-2-呋喃磺酰胺单钠盐 化合物 MCC950 sodium
  • 化合物 MCC950 sodium|T6887|TargetMol

化合物 MCC950 sodium|T6887|TargetMol

MCC950 sodium
256373-96-3
297 2mg 起订
483 5mg 起订
728 10mg 起订
上海 更新日期:2024-09-30

TargetMol中国(陶术生物)

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产品详情:

中文名称:
化合物 MCC950 sodium
英文名称:
MCC950 sodium
CAS号:
256373-96-3
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.12%
产品类别:
抑制剂
货号:
T6887

Product Introduction

Bioactivity

NameMCC950 sodium
DescriptionMCC950 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.
Cell ResearchMCC950 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].
Kinase Assaykinase 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.
Animal ResearchC57BL/6 mice were injected intraperitoneally with 50 mg/kg MCC950.
In vitro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]
In vivo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]
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationH2O : 42.7 mg/mL (100 mM)
DMSO : 55 mg/mL (128.97 mM)
KeywordsMCC 950 | MCC-950 sodium | inhibit | CP456773 | Inhibitor | NOD-like Receptor (NLR) | CRID3 | CP 456773 | MCC-950 | CRID 3 | CRID3 sodium | MCC950 sodium | CRID-3
Inhibitors RelatedBergenin | JC2-11 | Selnoflast | NLRP3-IN-2 | Imperatorin | INF39 | NLRP3-IN-10 | Dapansutrile | Stavudine | NOD-IN-1 | Muscone | Troxerutin
Related Compound LibrariesInhibitor Library | Pyroptosis Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Highly Selective Inhibitor Library | Anti-Aging Compound Library | HIF-1 Signaling Pathway Compound Library | Nonsteroidal Anti-Inflammatory Compound Library | Anti-Ovarian Cancer Compound Library | Antidepressant Compound Library
MCC950|||CRID3 sodium salt|||CP-456773 sodium|||CP-456773|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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