Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.91%
产品类别:
抑制剂
货号:
T2071
Product Introduction
Bioactivity
名称
MCOPPB triHydrochloride
描述
MCOPPB triHydrochloride (MCOPPB 3HCl) is a nociceptin receptor agonist.
激酶实验
Binding assay: Kinases are produced displayed on T7 phage or by expression in HEK-293 cells and tagged with DNA. Binding reactions are performed at room temperature for 1 hour, and the fraction of kinase not bound to test compound is determined by capture with an immobilized affinity ligand and quantitation by quantitative PCR. Each kinase is tested individually against CEP-32496. Kd values are determined using eleven serial 3-fold dilutions and presented as mean values from experiments performed in duplicate. Variability between individual values is less than 2-fold.
体内活性
仅有Parthenolide(一种具有抗炎特性的HDAC抑制剂)在Phb1 KO肝细胞中展现出显著的抗凋亡效应。实际上,经TSA和Parthenolide处理的肝细胞显示FXR水平升高,而CYP7A1、HDAC4、TNFα、TRAIL和Bax水平降低,这表明特定HDAC抑制作用导致胆汁酸的毒性效应减少,进而减轻了Phb1 KO肝细胞的凋亡反应。重要的是,Parthenolide在Phb1 KO小鼠BDL后的肝损伤中发挥保护作用。确实,Parthenolide治疗导致这些小鼠BDL后的死亡率降低,与对照的Phb1 KO小鼠相比,通过减少坏死区、Tunel染色以及ALT(8431±957 vs. 4225±210 U/L)和AST(4805±300 vs. 2242±438 U/L)活性的降低,揭示了较低的凋亡反应[3]。
存储条件
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.