1. Epigenetics
    PI3K/Akt/mTOR
  2. AMPK
  3. Buformin hydrochloride

Buformin hydrochloride (Synonyms: 1-Butylbiguanide hydrochloride)

Cat. No.: HY-B2099A
Handling Instructions

Buformin hydrochloride (1-Butylbiguanide hydrochloride) is a potent and orally active biguanide antidiabetic agent, an AMPK activator. Buformin hydrochloride decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin hydrochloride also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).

For research use only. We do not sell to patients.

Buformin hydrochloride Chemical Structure

Buformin hydrochloride Chemical Structure

CAS No. : 1190-53-0

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Estimated Time of Arrival: December 31
100 mg USD 75 In-stock
Estimated Time of Arrival: December 31
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Description

Buformin hydrochloride (1-Butylbiguanide hydrochloride) is a potent and orally active biguanide antidiabetic agent, an AMPK activator. Buformin hydrochloride decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin hydrochloride also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al)[1].

In Vitro

Buformin hydrochloride (0-10 mM; 5 days) inhibits SKBR3 and BT474 cells growth as a concentration-dependent manner, exhibits IC50 values of 246.7 μM and  98.6 μM for erbB-2-overexpressing SKBR3 and BT474 cells, respectively[1].
Buformin hydrochloride (0-3 mM; 48 hours)  increases the percentage of cells in G0/G1 phase and reduced the percentage of cells in S phase, especially in the SKBR3 cells[1].
Buformin hydrochloride (0-3 mM; 24 hours) suppresses RTK activation, including erbB-2 and IGF1R signaling  downstream, and Akt activation/phosphorylation is inhibited in both SKBR3 and BT474 cells[1].

Cell Viability Assay[1]

Cell Line: ErbB-2-overexpressing SKBR3 and BT474 cells
Concentration: 0 μM, 1 μM, 3 μM, 10 μM, 30 μM, 100 μM, 300 μM, 1, 3, or 10 mM
Incubation Time: 5 days
Result: Reduced cell viability in erbB-2-overexpressing breast cells.

Cell Cycle Analysis[1]

Cell Line: ErbB-2-overexpressing SKBR3 and BT474 cells
Concentration: 0.5 mM; 1 mM; 3 mM
Incubation Time: 48 hours
Result: Increased cells arresting in G0/G1 phase.

Western Blot Analysis[1]

Cell Line: ErbB-2-overexpressing SKBR3 and BT474 cells
Concentration: 0 mM, 0.1 mM, 0.3 mM, 1 mM, or 3 mM
Incubation Time: 24 hours
Result: Decreased p-AMPK, p-p706S, p-ERK1/2 expression in a concentration-dependent manner.
In Vivo

Buformin hydrochloride (oral administation; 7.6 mmol/kg of chow; 7 days) exhibits significantly reduced tumor volumes and weights, and hinders mammary morphogenesis and proliferation in MMTV-erbB-2 transgenic mice[1].

Animal Model: Female MMTV-erbB-2 transgenic mice[1]
Dosage: 7.6 mmol/kg
Administration: Oral administation; 7 days
Result: Inhibited mammary syngeneic tumor growth in MMTV-erbB-2 transgenic mice.
Molecular Weight

193.68

Formula

C₆H₁₆ClN₅

CAS No.

1190-53-0

SMILES

NC(NC(NCCCC)=N)=N.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (645.39 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.1632 mL 25.8158 mL 51.6316 mL
5 mM 1.0326 mL 5.1632 mL 10.3263 mL
10 mM 0.5163 mL 2.5816 mL 5.1632 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (10.74 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (10.74 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (10.74 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Buformin1-ButylbiguanideAMPKAMP-activated protein kinaseantidiabeticagentcervical cancerbreast cancerbiguanide analogType II diabeteSKBR3BT474Inhibitorinhibitorinhibit

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Buformin hydrochloride
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