Metformin HCl

For research use only. Not for use in humans.


Metformin HCl 化学構造


Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis).

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  • Cropped immunoblot analyses for downstream effector proteins of the MAPK and PI3K/AKT/mTOR signaling pathways for NRASQ61 mutant lung carcinoma and neuroblastoma cell lines. Dual pathway inhibition can be achieved by combining metformin and trametinib, as evidenced by the abolishment of p-ERK and p-S6.

    Oncotarget, 2015, 6(2): 969-78 . Metformin HCl purchased from Selleck.

  • Metformin added to atorvastatin therapy has no additional lipid-lowering effect. At the beginning of the experiment, rabbits were fed a high-cholesterol diet. After 2 weeks, rabbits were randomly stratified into the normal sodium (Ctrl group), atorvastatin (AT group), metformin (MT group), or atorvastatin/metformin combination therapy (AT + MT group) for a period of 10 weeks. Lipid levels were measured at −2, 0, 2, 6, 10 weeks after drug administration. Time-dependent changes and their AUC values of serum TC levels (A,B) are presented. Data are mean ± SD, n = 7 for each group. *P < 0.05, compared with Ctrl group. AUC, area under the curve; HDL-C, high-density lipoprotein cholesterol; LDL-C, low-density lipoprotein cholesterol; TC, total cholesterol.

    Sci Rep, 2017, 7(1):2169. Metformin HCl purchased from Selleck.


Carbohydrate Metabolism阻害剤の選択性比較


製品説明 Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis).
AMPK [1]

Metformin (500 μM) activates AMPK in hepatocytes, as a result, acetyl-CoA carboxylase (ACC) activity is reduced, fatty acid oxidation is induced, and expression of lipogenic enzymes is suppressed. Metformin (2 mM) activates muscle AMPK and promotes glucose uptake. Metformin (500 μM) or AICAR strongly suppresses SREBP-1 mRNA expression in rat hepatocytes. Metformin ameliorates hyperglycemia without stimulating insulin secretion, promoting weight gain, or causing hypoglycemia. Metformin has beneficial effects on circulating lipids linked to increased cardiovascular risk. Metformin decreases hepatic glucose production and increases skeletal myocyte glucose uptake. [1] Metformin requires LKB1 in the liver to lower blood glucose levels. [2] Metformin (2 mM) leads to a significant increase in the activity of both α1- and α2-containing complexes in muscle cells. Metformin (2 mM) also increases threonine 172 phosphorylation in muscle cells. [3]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HepG2 cells NWDYTZZTTnWwY4Tpc44h[XO|YYm= NVHje5RwOjRiaB?= NWDQTHdrUW6lcnXhd4UhcW5iZ3z1Z49{\SClb37zeY1xfGmxbjDpckBqdnO3bHnuMZJme2m|dHHueEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjCyOEBpenNuIFXDOVA:OC5{NzFOwG0v Ml;KNlE5PTZyNEi=
human MDA-MB-231 cells MY\GeY5kfGmxbjDhd5NigQ>? NELZSIgyKHSxIEKwJI1O NEjx[YYzPCCq MkHtRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG2IEGgeI8hOjBibV2gZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeT6= MVOyNlQ2QTJyOB?=
human HepG2 cells MkLESpVv[3Srb36gZZN{[Xl? M3zuZlEhdU1? M3u0TVI1KGh? MV7S[YR2[3Srb36gc4Yh\2y3Y3;z[UBkd26|dX3weIlwdiCrbjDpcpN2dGmwLYLld4l{fGGwdDDoeY1idiCKZYDHNkBk\WyuczDheEAyKG2PIHHmeIVzKDJ2IHjyd{BjgSCpbIXjc5NmKG:6aXThd4UhdWW2aH;kJIlvKHC{ZYPlcoNmKG:oIEKyMlIhdU1ib3[g[4x2[2:|ZR?= NGPYO3YzOzB{NUK0OC=>
mouse 3T3L1 cells NHqz[GFHfW6ldHnvckBie3OjeR?= M2H4XFEhdU1? MX3JcoR2[3Srb36gc4YhSU2SSzDwbI9{eGixconsZZRqd25iaX6gcY92e2ViM2SzUFEh[2WubIOgZZQhOSCvTTDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MVmyOVIyPjN5OR?=
human HepG2 cells NHXmdJJHfW6ldHnvckBie3OjeR?= MljINUBuVQ>? MkfvNlQhcA>? MmK5RYN1cX[jdHnvckBw\iCDTWDLJIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBodHWlb37lc4dmdmW|aYOgZZQhOSCvTTDh[pRmeiB{NDDodpMh[nliZX76fY1ifGmlIHPvcI9zcW2ndILpZ{Bie3OjeR?= NXziOnVxOjZ2N{GwPVA>


Methods Test Index PMID
Western blot
p-AMPK / AMPK / p-mTOR / mTOR / p-S6K / S6K; 

PubMed: 24505341     

The combined effects of metformin and heating were studied by heating the cells at 39.5–41°C for 1 h with 5 mM metformin and then incubating at 37°C for 47 h.

TTP / p-STAT3 / STAT3 / c-Myc ; 

PubMed: 26956973     

Metformin treatment increases phospho-AMPK (pAMPK) but decreases c-Myc and phospho-STAT3 (pSTAT3) in MCF7 and MDA-MB-231 cells. MCF7 and MDA-MB-231 cells were treated with 6 mM metformin for the indicated length of time, and the levels of TTP, STAT3, pSTAT3, AMPK, pAMPK, and c-Myc were measured by Western blotting.

pACC / ACC / pS6 / S6; 

PubMed: 26172303     

Western blot of pACC Ser79 (280 kDa), ACC (265 kDa), pS6 Ser240/244 (32 kDa), S6 (32 kDa), and β-actin (42 kDa) in HeyA8 cells treated with 0-5 mM metformin in normoglycemic or hyperglycemic conditions for 24 h.

pSTAT3 (Ser727) / STAT3 / Jak2 / Cdk5 / pNFκB / Bcl-2 / Bcl-XL / c-Myc; 

PubMed: 28114390     

Western blot of STAT3 and its regulatory proteins in Ishikawa cells after treatment with control, 10 mM, or 20 mM metformin for 48h in high-glucose conditions.

24505341 26956973 26172303 28114390

PubMed: 29601127     

LKB1 location with or without 10 lmol/L metformin treatment in Capan-2 wtLKB1 cell line. Scale bar, 50 μm.

PAR ; 

PubMed: 21422199     

A. MCF7 (left panel) or MDA-MB-231 (right panel) cells were treated with (Met) or without (Con) metformin for 2.5 days and then PAR (red) was detected by immunofluorescence using confocal microscopy. Nuclei (blue) were stained with DAPI.

CD86 / CD206; 

PubMed: 30899369     

Representative images of immunofluorescence analysis of macrophage phenotype in vitro, CD86 (M1 green) or CD206 (M2 red) were analysis. Scale bar 50 μm.

beta-catenin / AMPK; 

PubMed: 30854043     

Cells were treated with metformin for 24 h and subjected to immunofluorescence staining for β-catenin and AMPK. Magnification, ×400.

29601127 21422199 30899369 30854043
Growth inhibition assay
Cell viability ; 

PubMed: 26956973     

MCF7 and MDA-MB-231 cells were treated with the indicated concentrations of metformin for 24 h. Cell viability was assessed by measuring absorbance at 490 nm using an MTS cell proliferation assay. The values obtained with mock-treated cells were set to 100. Values are the mean ± SD (n = 3). *p < 0.05, **p < 0.01, ***p < 0.001.

体内試験 Metformin (100 mg/ml, po) treatment produces significant decreases in hepatic expression of mRNAs for SREBP-1, FAS, and S14 in SD rats that are consistent with effects documented in cells. Metformin also decreases hepatic lipids in obese mice. [1] Metformin (250 mg/kg, i.p.) increases AMPK phosphorylation in livers of wild-type mice. Metformin (250 mg/kg, i.p.) treatment reduces blood glucose by more than 50% in the wild-type mice on a high-fat diet. Metformin (250 mg/kg, i.p.) treatment also loweres blood glucose in the ob/ob mice by 40%. [2]


溶解度 (25°C)

体外 Water 33 mg/mL (199.25 mM) warming
DMSO Insoluble
Ethanol Insoluble

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。


分子量 165.62


CAS No. 1115-70-4
in solvent
別名 N/A
Smiles Cl.CN(C)C(=N)NC(N)=N





質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


質量 濃度 体積 分子量


NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03416127 Not yet recruiting Drug: Propolis|Drug: Metformin|Drug: Placebo Diabetes Mellitus Type 2 University of Guadalajara October 30 2019 Phase 2
NCT03710343 Not yet recruiting Drug: Metformin|Drug: Placebo Oral Tablet Cerebral Palsy|Spastic|Spastic Cerebral Palsy|Cerebral Palsy Spastic|Cerebral Palsy Mixed Holland Bloorview Kids Rehabilitation Hospital|The Hospital for Sick Children September 1 2019 Phase 2
NCT03994744 Recruiting Drug: PD-1 inhibitor|Drug: Metformin Small-cell Lung Cancer|Small Cell Lung Carcinoma|Small Cell Lung Cancer Recurrent|Small Cell Lung Cancer Extensive Stage Hunan Cancer Hospital|Xiangya Hospital of Central South University|Innovent Biologics (Suzhou) Co. Ltd. August 20 2019 Phase 2



Handling Instructions


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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID