Phenformin hydrochloride 是一种具有抗高血糖活性的双胍类抗糖尿病药物,能够使AMPK活化。
产品描述
Phenformin is an agent belonging to the biguanide class of antidiabetics with antihyperglycemic activity.
体外活性
在小鼠的肺脏和肺肿瘤中,Phenformin能够上调P-eIF2α和其靶标BiP/ Grp78的水平.
体内活性
在H441细胞中,Phenformin能够增加AMPK活性,同时降低基础离子的转运。在分离的心脏中,Phenformin 增加AMPK活性和磷酸化。在LKB1缺陷型NSCLC细胞系中,Phenformin 能够显著诱导凋亡。
激酶实验
Total AMPK activity is measured using the method of Dagher et al. AMPK activity is quantified in the resuspended pellet as incorporation of?32P from [γ-32P]ATP (10 GBq/mmol) into a synthetic peptide with the specific target sequence for AMPK, the SAMS peptide. Radioactivity is measured using a liquid scintillation counter. Protein content in the solution containing the resupended (NH4)2SO4 pellet is determined using the Bradford method.
Cas No.
834-28-6
分子式
C10H16ClN5
分子量
241.72
别名
Phenethylbiguanide hydrochloride;盐酸苯乙福明;Phenformin HCl
储存和溶解度
H2O:44 mg/mL (182 mM)
Ethanol:10 mg/mL (41.4 mM)
DMSO:45 mg/mL (186.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years