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：2024-12-12

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

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.
溶解度	H2O : 42.7 mg/mL (100 mM) DMSO : 55 mg/mL (128.97 mM)
关键字	MCC 950 \| MCC-950 sodium \| inhibit \| CP456773 \| Inhibitor \| NOD-like Receptor (NLR) \| CRID3 \| CP 456773 \| MCC-950 \| CRID 3 \| CRID3 sodium \| MCC950 sodium \| CRID-3
相关产品	Bergenin \| JC2-11 \| Selnoflast \| NLRP3-IN-2 \| Imperatorin \| INF39 \| NLRP3-IN-10 \| Dapansutrile \| Stavudine \| NOD-IN-1 \| Muscone \| Troxerutin
相关库	抑制剂库 \| 细胞焦亡化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 高选择性抑制剂库 \| 抗衰老化合物库 \| HIF-1化合物库 \| 非甾体类抗炎化合物库 \| 抗卵巢癌化合物库 \| 抗抑郁症化合物库

MCC950|||CRID3 sodium salt|||CP-456773 sodium|||CP-456773|TargetMol

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