MCC950

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Chemical Structure| 210826-40-7 同义名 : CP-456773; CRID3
CAS号 : 210826-40-7
货号 : A448777
分子式 : C20H24N2O5S
纯度 : 99%
分子量 : 404.48
MDL号 : MFCD28900720
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 The NOD-like receptor family protein NLRP3 is an intracellular signaling molecular that forms a complex termed inflammasome with other proteins during inflammatory process, which promotes the release of proinflammatory cytokines, such as IL-1β and IL-18. MCC950 is a potent and selective inhibitor of NLRP3. It inhibits the release of IL-1β with IC50 values of 7.5 nM in mouse bone marrow derived macrophages (BMDM) and 8.1 nM in human monocyte derived macrophages. The amount of caspase-1 p10 was reduced in the supernatants of BMDM and human peripheral blood mononuclear cells (PBMC) after the treatment of 10 and 50 nM MCC950. In BMDM stimulated by LPS and nigericin, MCC950 from 0.1 – 10 μM potently inhibited the release of IL-1α and lactate dehydrogenase. Pre-treatment of 0.01 – 1 μM MCC950 before the transfection of LPS dose-dependently inhibited the release of IL-β in BMDM. The expression of ASC complex was blocked by 10 and 50 nM MCC950 in LPS- and nigericin-treated BMDM. The amount of ASC-cerulean cells containing an ASC speck was dose-dependently decreased by the pre-treatment of 0.05 – 10 μM MCC950. Pre-treatment of MCC950 (50 mg/kg) one hour before the intraperitoneal injection of LPS in C57BL/6 mice decreased the serum concentration of IL-1β and IL-6. Treatment of MCC950 (10 mg/kg, i.p.) postponed the onset and attenuated the severity of EAE in C57BL/6 mice. MWS mice that received i.p. administration of MCC950 (20 mg/kg) showed increased body weight, elevated survival rate and reduced concentration of circulating IL-18[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.36mL

2.47mL

1.24mL

24.72mL

4.94mL

2.47mL
参考文献

[1]Gan W, Ren J, et al. The SGK1 inhibitor EMD638683, prevents Angiotensin II-induced cardiac inflammation and fibrosis by blocking NLRP3 inflammasome activation. Biochim Biophys Acta. 2017 Oct 3;1864(1):1-10.

[2] Coll RC, Robertson AA, Chae JJ, Higgins SC, Muñoz-Planillo R, Inserra MC, Vetter I, Dungan LS, Monks BG, Stutz A, Croker DE, Butler MS, Haneklaus M, Sutton CE, Núñez G, Latz E, Kastner DL, Mills KH, Masters SL, Schroder K, Cooper MA, O'Neill LA. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nat Med. 2015 Mar;21(3):248-55. doi: 10.1038/nm.3806. Epub 2015 Feb 16. PMID: 25686105; PMCID: PMC4392179.