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- Phenformin HCl
Phenformin HCl
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 241.72 |
| Cas No. | 834-28-6 |
| Formula | C10H16ClN5 |
| Solubility | ≥12.1 mg/mL in DMSO; ≥17.53 mg/mL in EtOH; ≥24.5 mg/mL in H2O with ultrasonic |
| Chemical Name | 1-(diaminomethylidene)-2-(2-phenylethyl)guanidine;hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | C1=CC=C(C=C1)CCN=C(N)N=C(N)N.Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
BRAFV600E Me-1 melanoma cells and HEK-293 cells |
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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. |
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Reacting condition |
1 or 5 mM; 2 hrs |
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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]: | |
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Animal models |
Tyr::CreER; BRAFCA/+; PTENlox/lox mice bearing single tumor induced by 4-HT |
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Dosage form |
100 mg/kg; p.o.; b.i.d. |
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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. |
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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. |
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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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Quality Control & MSDS
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Chemical structure
