MCC950 (sodium salt)

一种NLRP3炎症体激活抑制剂；在1µM浓度下抑制脂多糖（LPS）预处理的小鼠骨髓来源巨噬细胞（BMDMs）中由ATP诱导的IL-1β释放（IC50=7.5nM），同时在Pam3CSK4预处理的小鼠BMDMs中抑制细胞质LPS诱导的IL-1β释放（0.1µM和1µM）；对NLRP3的选择性高于NLRC4和AIM2炎症体，并且在10µM浓度下不抑制小鼠BMDMs中LPS诱导的NLRP3预激活；在1µM浓度下减少氧化型低密度脂蛋白（ox-LDL）诱导的caspase-1活性增加，并抑制THP-1巨噬细胞中的焦亡；在小鼠左冠状动脉结扎诱导的心肌梗死后，以10mg/kg剂量给药可减少心肌纤维化；在小鼠脊髓压迫损伤模型中，以10 mg/kg剂量给药可改善前肢抓握力并减少脊髓水肿。An inhibitor of NLRP3 inflammasome activation; inhibits ATP-induced IL-1β release in LPS-primed mouse BMDMs (IC50 = 7.5 nM), as well as cytosolic LPS-induced IL-1β release in Pam3CSK4-primed mouse BMDMs at 0.1 and 1 µM; selective for NLRP3 over NLRC4 and AIM2 inflammasomes and does not inhibit LPS-induced NLRP3 priming in mouse BMDMs at 10 µM; reduces ox-LDL-induced increases in caspase-1 activity and inhibits pyroptosis in THP-1 macrophages at 1 µM; reduces myocardial fibrosis in mice following myocardial infarction induced by left coronary artery ligation at 10 mg/kg; improves forelimb grip strength and reduces spinal edema in a mouse model of spinal crush injury at 10 mg/kg.分子式C20H23N2O5S • Na分子量426.5O=C([N-]S(=O)(C1=CC(C(C)(O)C)=CO1)=O)NC2=C(CCC3)C3=CC4=C2CCC4.[Na+]