黑皮质素MC4受体拮抗剂,ML00253764 is a non-peptide, brain penetrant melanocortin MC4 receptor (MC4R) antagonist with IC50 of 0.32, 0.81 and 2.12 uM for MC4, MC3 and MC5 receptors, respectively
黑皮质素MC4受体拮抗剂,ML00253764 is a non-peptide, brain penetrant melanocortin MC4 receptor (MC4R) antagonist with IC50 of 0.32, 0.81 and 2.12 uM for MC4, MC3 and MC5 receptors, respectively
生物活性
ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity.
性状
Solid
体外研究(In Vitro)
ML00253764(0.001-50 μM, 24 h or 72 h)对人胶质母细胞瘤细胞增殖具有显著的时间和浓度依赖性抑制活性,其中作用于 U-118 细胞的 IC50 值为 6.56 μM,可以诱导U-87细胞凋亡,且在这两种细胞系中均表现出显著的 ERK1/2 磷酸化抑制作用。
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.