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    Phenformin HCl
    Phenformin HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0247
    CAS #: 834-28-6Purity ≥98%

    Description: Phenformin HCl, a hydrochloride salt of phenformin, is an anti-diabetic drug belonging to the biguanide class. It is potent to lower blood glucose concentrations in patients with non-insulin-dependent diabetes mellitus. Phenformin Hydrochloride improves insulin sensitivity and decrease insulin resistance by inhibiting complex 1 of the mitochondrial respiratory chain and inducing AMP-activated protein kinase (AMPK)-dependent signaling. 

    References:Am J Physiol Heart Circ Physiol. 2007 Jul;293(1):H457-66; Diabetologia. 1975 Oct;11(5):475-82.

    Related CAS #: 834-28-6 (HCl); 114-86-3 (free base) 

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    Molecular Weight (MW)

    241.72

    Formula

    C10H15N5.HCl

    CAS No.

    834-28-6

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 48 mg/mL (198.6 mM)

    Water: 48 mg/mL (198.6 mM)

    Ethanol: 12 mg/mL (49.6 mM)

    Solubility (In vivo)

    Chemical Name: 1-(diaminomethylidene)-2-(2-phenylethyl)guanidine;hydrochloride

    InChi Key: YSUCWSWKRIOILX-UHFFFAOYSA-N

    InChi Code: InChI=1S/C10H15N5.ClH/c11-9(12)15-10(13)14-7-6-8-4-2-1-3-5-8;/h1-5H,6-7H2,(H6,11,12,13,14,15);1H

    SMILES Code: C1=CC=C(C=C1)CCN=C(N)N=C(N)N.Cl

    Synonyms

    W-104144; ST-50409947; D-08352; W104144; ST50409947; D08352; W 104144; ST 50409947; D 08352; Phenformin Hydrochloride; Phenformin HCl; Meltrol; Dipar; Phenethylbiguanide hydrochloride; 


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    In Vitro

    In vitro activity: Phenformin stimulates the phosphorylation and activation of AMPKalpha1 and AMPKalpha2 without altering LKB1 activity. 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]. 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. 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. Phenformin-treated rats reveals a tendency towards a decrease in blood insulin level (radioimmunoassay).

     

    Kinase Assay: Total AMPK activity is measured using the method of Dagher et al. AMPK activity is quantified in the resuspended pellet as incorporation of 32P from [γ-32P]ATP (10 GBq/mmol) into a synthetic peptide with the specific target sequence for AMPK, the SAMS peptide. Radioactivity is measured using a liquid scintillation counter. Protein content in the solution containing the resupended (NH4)2SO4 pellet is determined using the Bradford method.

     

    Cell Assay: 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).

    In Vivo

    Phenformin also increases levels of P-eIF2α and its target BiP/Grp78 in normal lung as well as in lung tumors of mice.

    Animal model

    Mice

    Formulation & Dosage

    N/A

    References

    Am J Physiol Heart Circ Physiol. 2007 Jul;293(1):H457-66; Diabetologia. 1975 Oct;11(5):475-82.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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