AICAR 是一种腺苷类似物,是一种 AMP 激活的蛋白激酶激活剂,可用于治疗急性淋巴细胞白血病和糖尿病。
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Acadesine is an AMP-activated protein kinase activator which is used for the treatment of acute lymphoblastic leukemia and may have applications in treating other disorders such as diabetes.
体外活性
在猪体内, Acadesine(10 mg/kg)抑制肺毛细血管中脂多糖诱导的蛋白渗透,
体内活性
在大鼠肝细胞中, Acadesine(500 μM)能够引起MPK的短暂活化,显着抑制大鼠肝细胞脂肪酸和甾醇的合成,同时引起HMG-CoA还原酶失活。B-CLL细胞中(EC50=380 μM),Acadesine(0.5 mM)能够诱导B-CLL细胞凋亡并激活AMPK。
细胞实验
Acadesine is added to K562 cell lines or primary cells (103 CD34+ cells/mL) growing in semisolid methyl cellulose medium. MethoCult H4100 or H4236 are used for cell lines and primary CD34+ cells respectively. Colonies are detected after 10 days of culture by adding 1 mg/mL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reagent and are scored by Image J quantification software. (Only for Reference)
Cas No.
2627-69-2
分子式
C9H14N4O5
分子量
258.234
别名
NSC105823;AICA Riboside;Acadesine;阿卡地新;AICAR (Acadesine)
储存和溶解度
DMSO:19.4 mg/mL (75 mM)
H2O:19.4 mg/mL (75 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years