产品
编 号:F134633
分子式:C20H21Cl2N3OS
分子量:422.37
产品类型
结构图
CAS No: 1354030-52-6
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产品详情
生物活性:
UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions.
体内研究:
UNC9995(2 mg/kg/天,腹腔注射,2 周)在小鼠的慢性社交失败应激 (CSDS) 模型和慢性不可预知轻度应激 (CUMS) 模型中,改善了抑郁样行为表型并改善海马体中星形胶质细胞的丢失。Animal Model:Chronic unpredictable mild stress (CUMS) mouse model
Dosage:2 mg/kg/d
Administration:IP; 2 weeks
Result:Improved depressive-like symptoms of CUMS mouse model in WT mice but not Arrb2?/? mice.
体外研究:
UNC9995(10 μM;1 小时)预处理原代星形胶质细胞,使它受IL-6(300 ng/mL;24 小时)诱导后,STAT3 和 β-arrestin2 的结合得到增强。它还抑制 STING、TBK1、JAK 的激活。UNC9995(1、5、10 和 20 μM;1 小时)能够消除细胞凋亡和炎症,当用 IL-6 (300 ng/mL;24 小时) 刺激 WT 和 Arrb2?/? 星形胶质细胞后。