MCC950 sodium NEW
| Price | $30 | $47 | $76 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-18 |
Product Details
| Product Name: MCC950 sodium | CAS No.: 256373-96-3 |
| Purity: 99.12% | Supply Ability: 10g |
| Release date: 2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | 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. |
| 細(xì)胞實(shí)驗(yàn) | 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]. |
| 激酶實(shí)驗(yàn) | 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. |
| 動物實(shí)驗(yàn) | C57BL/6 mice were injected intraperitoneally with 50 mg/kg MCC950. |
| 體外活性 | METHODS: Mouse bone marrow-derived macrophages BMDM were stimulated with LPS (10 ng/mL) for 3 h, stimulated with MCC950 sodium (1-1000 nM) for 30 min, and then treated with ATP (5 mM) for 1 h. Levels of IL-1β and TNF-α were measured by ELISA. RESULTS: MCC950-treated cells dose-dependently inhibited the release of IL-1β in BMDM, and LPS-dependent TNF-α secretion was not impaired by MCC950. [1] MCC950 was used in the treatment of BMDM cells. METHODS: Mouse macrophages, human coronary artery endothelial cells and smooth muscle cells were treated with MCC950 sodium (0.02-20 μM) for 3 days, and cell viability was measured by Alamar Blue assay. RESULTS: MCC950 sodium had no toxic effect on the three cells. [2] |
| 體內(nèi)活性 | METHODS: To detect anti-NLRP3 activity in vivo, MCC950 sodium (20 mg/kg) was injected intraperitoneally into a mouse model of the human CAPS disease MWS once daily for four weeks. RESULTS: MCC950 rescued the CAPS mouse model and inhibited NLRP3 in human MWS cells. [1] METHODS: To investigate the pharmacological effects on experimental spinal cord injury models in vivo and neuronal injury in vitro, MCC950 sodium (10-50 mg/kg) was intraperitoneally injected into C57BL/6 mice with spinal cord injury (SCI). RESULTS: MCC950 improved grip strength, hindlimb movement, spinal cord edema, and pathological damage in SCI mice. It exerted this effect by blocking NLRP3 inflammatory vesicle assembly and the release of the pro-inflammatory cytokines TNF-α, IL-1β, and IL-18. [3] |
| 存儲條件 | 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) |
| 關(guān)鍵字 | 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 |
| 相關(guān)產(chǎn)品 | Stavudine | Dapansutrile | NOD-IN-1 | Imperatorin | Muscone | NLRP3-IN-2 | Bergenin | Troxerutin | NLRP3-IN-9 | INF39 | Selnoflast | JC2-11 |
| 相關(guān)庫 | 高選擇性抑制劑庫 | 表型篩選靶點(diǎn)鑒定庫 | 經(jīng)典已知活性庫 | 抑制劑庫 | 抗前列腺癌化合物庫 | NO PAINS 化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌化合物庫 | 抗肝癌化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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