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CAS No.: 210826-40-7

MCC950 Catalog No. CSN18104

Synonyms: CP-456773;CRID3;CP 456,773

MCC950 is a potent, selective, small-molecule inhibitor of NLRP3 with IC50 of 7.5 nM in BMDMs.

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实验方案

技术信息

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].
动物研究
剂量
Mice: 10 mg/kg^[3] (i.p.), 50 mg/kg^[4] (i.p.); 2 mg/kg - 10 mg/kg^[5] (s.c.); 50 mg/kg^[6] (p.o.) Rat: 3 mg/kg (i.v.)

给药途径
i.p., s.c., i.v., p.o.
参考文献

动物研究
剂量	Mice: 10 mg/kg^[3] (i.p.), 50 mg/kg^[4] (i.p.); 2 mg/kg - 10 mg/kg^[5] (s.c.); 50 mg/kg^[6] (p.o.) Rat: 3 mg/kg (i.v.)
给药途径	i.p., s.c., i.v., p.o.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4723 mL
- 12.3616 mL
- 24.7231 mL
- 5 mM
- 0.4945 mL
- 2.4723 mL
- 4.9446 mL
- 10 mM
- 0.2472 mL
- 1.2362 mL
- 2.4723 mL

技术信息

CAS号	210826-40-7	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C20H24N2O5S	运输	蓝冰
分子量	404.48	别名	CP-456773;CRID3;CP 456,773

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