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Phenformin hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Phenformin hydrochloride图片
CAS NO:834-28-6
包装与价格:
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

产品名称
盐酸苯乙福明
Phenethylbiguanide hydrochloride
产品介绍
Phenformin hydrochloride 是一种双胍类的抗糖尿病药,能够使AMPK活化。
生物活性

Phenformin hydrochloride is an anti-diabetic drug from the biguanide class, can activateAMPKactivity.

IC50& Target[2]

AMPK

 

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.1370 mL20.6851 mL41.3702 mL
5 mM0.8274 mL4.1370 mL8.2740 mL
10 mM0.4137 mL2.0685 mL4.1370 mL
*

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
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

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
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 2.5 mg/mL (10.34 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

  • 2.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 0.42 mg/mL (1.74 mM); Clear solution

    此方案可获得 ≥ 0.42 mg/mL (1.74 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 4.2 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 0.42 mg/mL (1.74 mM); Clear solution

    此方案可获得 ≥ 0.42 mg/mL (1.74 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 4.2 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 0.42 mg/mL (1.74 mM); Clear solution

    此方案可获得 ≥ 0.42 mg/mL (1.74 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 4.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。