Buformin hydrochloride 是一种有效的 AMPK 激活剂,是一种双胍类的口服抗糖尿病药物。Buformin 延缓胃肠道对葡萄糖的吸收,增加胰岛素敏感性和葡萄糖对细胞的吸收,并抑制肝脏对葡萄糖的合成。Buformin 也具有抗癌活性,可用于各种癌症研究。
产品描述
Buformin hydrochloride is a potent AMPK activator,an oral antidiabetic drug of the biguanide class. Buformin delays the absorption of glucose from the gastrointestinal tract increases insulin sensitivity and glucose uptake into cells and inhibits synthesis of glucose by the liver. Biguanides may antagonize the action of glucagon, thus reducing fasting glucose levels.
体外活性
Buformin hydrochloride (0-10 mM; 5 days) inhibits SKBR3 and BT474 cells growth as a concentration-dependent manner, exhibits IC50 values of 246.7 μM and ?98.6 μM for erbB-2-overexpressing SKBR3 and BT474 cells, respectively[1].
Buformin hydrochloride (0-3 mM; 48 hours) increases the percentage of cells in G0/G1 phase and reduced the percentage of cells in S phase, especially in the SKBR3 cells[1].
Buformin hydrochloride (0-3 mM; 24 hours) suppresses RTK activation, including erbB-2 and IGF1R signaling downstream, and Akt activation/phosphorylation is inhibited in both SKBR3 and BT474 cells[1].
体内活性
Buformin hydrochloride (oral administation; 7.6?mmol/kg of chow; 7 days) exhibits significantly reduced tumor volumes and weights, and?hinders mammary morphogenesis and proliferation in MMTV-erbB-2 transgenic mice[1].
Cas No.
1190-53-0
分子式
C6H16ClN5
分子量
193.68
别名
NSC528218;盐酸丁双胍;NSC 528218;NSC-528218
储存和溶解度
DMSO:60 mg/ml (309.79 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years