CAS NO: | 834-28-6 |
包装 | 价格(元) |
10 mM * 1 mL in Water | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
10 g | 电议 |
50 g | 电议 |
生物活性 | Phenformin hydrochloride is an anti-diabetic drug from the biguanide class, can activateAMPKactivity. | ||||||||||||||||
IC50& Target[2] |
| ||||||||||||||||
体外研究 (In Vitro) | Phenformin stimulates the phosphorylation and activation of AMPKalpha1 and AMPKalpha2 without altering LKB1 activity[1]. Phenformin increases AMPK activity and phosphorylation in the isolated heart, the increase in AMPK activity is always preceded by and correlated with increased cytosolic [AMP][2]. Phenformin is a 50-fold more potent inhibitor of mitochondrial complex I than metformin. Phenformin robustly induces apoptosis in LKB1 deficient NSCLC cell lines. Phenformin at 2 mM similarly induces AMPK signaling as shown by increased P-AMPK and P-Raptor levels. Phenformin induces higher levels of cellular stress, triggering induction of P-Ser51 eIF2α and its downstream target CHOP, and markers of apoptosis at later times. Phenformin induces a significant increase in survival and therapeutic response in KLluc mice following long-term treatment[3]. Phenformin and AICAR increases AMPK activity in H441 cells in a dose-dependent fashion, stimulating the kinase maximally at 5-10 mm and 2 mm, respectively. Phenformin significantly decreases basal ion transport (measured as short circuit current) across H441 monolayers by approximately 50% compared with that of controls. Phenformin and AICAR significantly reduce amiloride-sensitive transepithelial Na+ transport compared with controls. Phenformin and AICAR suppress amiloride-sensitive Na+transport across H441 cells via a pathway that includes activation of AMPK and inhibition of both apical Na+ entry through ENaC and basolateral Na+extrusion via the Na+,K+-ATPase[4]. Phenformin-treated rats reveals a tendency towards a decrease in blood insulin level (radioimmunoassay)[5]. | ||||||||||||||||
体内研究 (In Vivo) | Phenformin increases levels of P-eIF2α and its target BiP/Grp78 in normal lung as well as in lung tumors of mice[3]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 241.72 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C10H16ClN5 | ||||||||||||||||
CAS 号 | 834-28-6 | ||||||||||||||||
中文名称 | 盐酸苯乙福明 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) | ||||||||||||||||
溶解性数据 | In Vitro: H2O : 12.5 mg/mL(51.71 mM;Need ultrasonic) Ethanol : 2 mg/mL(8.27 mM;Need ultrasonic) DMSO : 1 mg/mL(4.14 mM;ultrasonic and adjust pH to 2 with 1M HCl) DMF : 1 mg/mL(4.14 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
|