MCC950 sodium

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Chemical Structure| 256373-96-3 同义名 : CP-456773 sodium;CRID3 sodium salt;CP 456,773;MCC950 (sodium salt);CRID3 Sodium
CAS号 : 256373-96-3
货号 : A110681
分子式 : C20H23N2NaO5S
纯度 : 99%+
分子量 : 426.462
MDL号 : MFCD30478884
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(246.21 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 30 mg/mL(70.35 mM)
动物实验配方：

PO 0.5% CMC-Na 40 mg/mL suspension

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 sodium 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[1].
作用机制 MCC950 sodium might have an inhibitory effect on a critical step in NLRP3 activation at post-translational level[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.72mL

2.34mL

1.17mL

23.45mL

4.69mL

2.34mL
参考文献

[1]Coll RC, Robertson AA, et al. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nat Med. 2015;21(3):248-55.

[2]Wu D, Wu K, et al. Formononetin Administration Ameliorates Dextran Sulfate Sodium-Induced Acute Colitis by Inhibiting NLRP3 Inflammasome Signaling Pathway. Mediators Inflamm. 2018 Jan 8;2018:3048532.

[3]Ludwig-Portugall I, Bartok E, et al. An NLRP3-specific inflammasome inhibitor attenuates crystal-induced kidney fibrosis in mice. Kidney Int. 2016 Sep;90(3):525-39.

[4]Gordon R, Albornoz EA, et al. Inflammasome inhibition prevents α-synuclein pathology and dopaminergic neurodegeneration in mice. Sci Transl Med. 2018 Oct 31;10(465). pii: eaah4066