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Phenformin HCl

Catalog No.
B1373
biguanidine drug with anti-diabetic activity
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$80.00
In stock
50mg
$40.00
In stock
10g
$50.00
In stock
50g
$150.00
In stock

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Background

Phenformin HCl is a hydrochloride salt of the biguanidine drug phenformin.
Phenformin is the biguanide class that displays anti-diabetic activity.
In 5 patients with diabetes mellitus, phenformin reduced the blood glucose values and glycosuria. In 4 of 5 patients, cholesterol and total lipid levels were dropped. Also, Phenformin had no impact on glucose, nor the insulin levels after intravenous glucose loading.
References:
[1]. Geldermans CA, Terpstra J, Krans HM. The effect of phenformin-HCl on patients with diabetes mellitus, studied under strict balance conditions. Diabetologia, 1975, 11(5): 475-482.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt241.72
Cas No.834-28-6
FormulaC10H16ClN5
Solubility≥12.1mg/mL in DMSO
Chemical Name1-(diaminomethylidene)-2-(2-phenylethyl)guanidine;hydrochloride
SDFDownload SDF
Canonical SMILESC1=CC=C(C=C1)CCN=C(N)N=C(N)N.Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

BRAFV600E Me-1 melanoma cells and HEK-293 cells

Preparation method

The solubility of this compound in DMSO is > 12.1 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

1 or 5 mM; 2 hrs

Applications

In BRAFV600E Me-1 melanoma cell line (with impaired AMPK activation), 1 and 5 mM Phenformin significantly increased AMPK kinase activity, in a dose-dependent manner. A similar increase was also observed in HEK-293 cells (as control cells). These results implied that the presence of BRAFV600E in melanoma cells did not prevent the pharmacological activation of AMPK, and that AMPK was activated by the increase in phosphorylation of a key AMPK downstream target (ACC).

Animal experiment [2]:

Animal models

Tyr::CreER; BRAFCA/+; PTENlox/lox mice bearing single tumor induced by 4-HT

Dosage form

100 mg/kg; p.o.; b.i.d.

Applications

In Tyr::CreER; BRAFCA/+; PTENlox/lox mice bearing single tumor induced by 4-HT, the combination of Phenformin and PLX4720 significantly inhibited tumor growth. PLX4720 alone substantially reduced the rate of tumor progression, but Phenformin alone only showed a modest inhibition on tumor growth in these mice. According to immunohistochemical analyses of these tumors, the Phenformin/PLX4720 combination dramatically promoted apoptotic cell death and inhibited tumor cell proliferation.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Petti C, Vegetti C, Molla A, Bersani I, Cleris L, Mustard KJ, Formelli F, Hardie GD, Sensi M, Anichini A. AMPK activators inhibit the proliferation of human melanomas bearing the activated MAPK pathway. Melanoma Res. 2012 Oct;22(5):341-50.

[2]. Yuan P, Ito K, Perez-Lorenzo R, Del Guzzo C, Lee JH, Shen CH, Bosenberg MW, McMahon M, Cantley LC, Zheng B. Phenformin enhances the therapeutic benefit of BRAF(V600E) inhibition in melanoma. Proc Natl Acad Sci U S A. 2013 Nov 5;110(45):18226-31.

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