Metformin HCl

製品コードS1950

Metformin HCl 化学構造

分子量(MW):165.62

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

サイズ 価格(税別)  
JPY 18100
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カスタマーフィードバック(2)

  • 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.

製品安全説明書

Carbohydrate Metabolism阻害剤の選択性比較

生物活性

製品説明 Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis).
ターゲット
AMPK [1]
(Hepatocytes)
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HepG2 cells MWHGeY5kfGmxbjDhd5NigQ>? NYfKfXBmOjRiaB?= MVrJcoNz\WG|ZTDpckBodHWlb4PlJINwdnO3bYD0bY9vKGmwIHnud5VtcW5vcnXzbZN1[W62IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDJ2IHjyd{whTUN3ME2wMlI4KM7:TT6= Ml\hNlE5PTZyNEi=
human MDA-MB-231 cells Ml6wSpVv[3Srb36gZZN{[Xl? NGPBPFgyKHSxIEKwJI1O Mn:3NlQhcA>? NIfrSWRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYSgNUB1dyB{MDDtUUBi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5Mi=> Mk\ONlI1PTl{MEi=
human HepG2 cells MnrzSpVv[3Srb36gZZN{[Xl? MUOxJI1O MnqyNlQhcA>? NGDUSHhT\WS3Y4Tpc44hd2ZiZ3z1Z49{\SClb37zeY1xfGmxbjDpckBqdnO3bHnuMZJme2m|dHHueEBpfW2jbjDI[ZBIOiClZXzsd{BifCBzIH3NJIFnfGW{IEK0JIhzeyCkeTDncJVkd3OnIH;4bYRie2VibXX0bI9lKGmwIIDy[ZNmdmOnIH;mJFIzNjJibV2gc4Yh\2y3Y3;z[S=> NI\GTYMzOzB{NUK0OC=>
mouse 3T3L1 cells MkXKSpVv[3Srb36gZZN{[Xl? NFnlRnIyKG2P MVzJcoR2[3Srb36gc4YhSU2SSzDwbI9{eGixconsZZRqd25iaX6gcY92e2ViM2SzUFEh[2WubIOgZZQhOSCvTTDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? M2HHV|I2OjF4M{e5
human HepG2 cells M1;EeGZ2dmO2aX;uJIF{e2G7 NF3sbIEyKG2P NHr6bnAzPCCq NF\pXXpC[3SrdnH0bY9vKG:oIFHNVGshcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGeudXPvcoVw\2WwZYPpd{BifCBzIH3NJIFnfGW{IEK0JIhzeyCkeTDlcpp6dWG2aXOgZ49td3KrbXX0dolkKGG|c3H5 NYfmU5l4OjZ2N{GwPVA>

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アッセイ
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
Immunofluorescence
LKB1; 

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.

26956973
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]

お薦めの試験操作(参考用のみ)

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。

化学情報

分子量 165.62
化学式

C4H11N5.HCl

CAS No. 1115-70-4
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

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

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

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

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03686657 Not yet recruiting Type 2 Diabetes|High Blood Pressure|Arthritis|Obesity ARKAY Therapeutics|Albany Medical College August 5 2019 Phase 1|Phase 2
NCT03499704 Not yet recruiting Diabetes Mellitus Type 2 Takeda August 31 2019 Phase 4
NCT03499704 Not yet recruiting Diabetes Mellitus Type 2 Takeda August 31 2019 Phase 4
NCT03686657 Not yet recruiting Type 2 Diabetes|High Blood Pressure|Arthritis|Obesity ARKAY Therapeutics|Albany Medical College August 5 2019 Phase 1|Phase 2
NCT03452267 Not yet recruiting Insulin Sensitivity Wayne State University June 2019 Phase 2|Phase 3
NCT03452267 Not yet recruiting Insulin Sensitivity Wayne State University June 2019 Phase 2|Phase 3

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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