Size | Price | Stock | Qty |
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500mg |
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1g |
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2g |
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5g |
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10g |
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25g |
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Other Sizes |
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Purity: ≥98%
Targets |
AMPK; JNK; p38 MAPK
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ln Vitro |
Metformin inhibits Bcl-2 and Bcl-xl, upregulates BAX activation with facilitation of BIM, BAD, and PUMA, and induces release of cytochrome c from mitochondria into the cytoplasm, directly inducing caspase-9-mediated mitochondrial apoptosis.[4]
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ln Vivo |
Metformin exhibits a therapeutic effect in a mouse model of nonalcoholic steatohepatitis (NASH)-related liver fibrosis, resulting in improvements in hepatic function, NASH lesions, and fibrosis.[4]
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Enzyme Assay |
This study demonstrates that metformin decreased the number of activated-HSCs through induction of apoptosis, but did not impact numbers of hepatocytes. Metformin upregulated BAX activation with facilitation of BIM, BAD and PUMA; downregulated Bcl-2 and Bcl-xl, but did not affect Mcl-1. Additionally, metformin induced cytochrome c release from mitochondria into the cytoplasm, directly triggering caspase-9-mediated mitochondrial apoptosis. The decline in mitochondrial membrane potential (ΔΨm) and deposition of superoxide in mitochondria accelerated the destruction of the integrity of mitochondrial membrane. Moreover, we verified the therapeutic effect of metformin in our mouse model of liver fibrosis associated with nonalcoholic steatohepatitis (NASH) in which hepatic function, NASH lesions and fibrosis were improved by metformin. In conclusion, this study indicated that metformin has significant therapeutic value in NASH-derived liver fibrosis by inducing apoptosis in HSCs, but does not affect the proliferation of hepatocytes [4].
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Cell Assay |
Rat HSCs T6, human hepatocyte L02, and rat hepatocyte BRL-3A were maintained in DMEM, which is supplemented with 10% (v/v) FBS and 1% (v/v) penicillin/streptomycin sulfate at 37 °C in a humidified 5% CO2 incubator. The human hepatic stellate cells (HSCs) LX-2 are maintained in RPMI 1640 medium. Filtered through millipore membrane filters with a 0.22 m pore size are solutions of metformin and AICAR. The CCK8 assay is used to measure the effects of various metformin and AICAR concentrations on the growth of hepatic stellate cells. Following a 24-hour treatment with varying doses of metformin and AICAR, the expression of collagen and -SMA protein is discovered using a Western blot. After giving cells 10 mM metformin and 0.5 mM AICAR for 24 hours, Western blot is used to identify the expression of collagen and the -SMA protein. RT-qPCR is used to find the mRNA levels of collagen I and -SMA.
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Animal Protocol |
Male C57BL/6N mice
10-200 mg/kg; 65 mg/kg i.p. |
References |
Molecular Formula |
C4H11N5
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Molecular Weight |
129.17
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Exact Mass |
129.1014
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Elemental Analysis |
C, 37.20; H, 8.58; N, 54.22
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CAS # |
657-24-9
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Related CAS # |
Metformin hydrochloride;1115-70-4 (HCl); 657-24-9;1384526-74-2 (icosapent); 58840-24-7 (orotate); 121369-64-0 (glycinate); 34461-22-8 ( embonate)
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Appearance |
White to light yellow solid powder
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LogP |
-2.31
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tPSA |
88.99
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SMILES |
CN(C)C(=N)N=C(N)N
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InChi Key |
XZWYZXLIPXDOLR-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C4H11N5/c1-9(2)4(7)8-3(5)6/h1-2H3,(H5,5,6,7,8)
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Chemical Name |
3-(diaminomethylidene)-1,1-dimethylguanidine
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Synonyms |
Fluamine; Flumamine; LA6023; LA-6023; LA 6023; Metformin; Metiguanide; Diabetosan; Diabex; Dimethylbiguanide; DMGG
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 25~26 mg/mL (193.6~201.3 mM)
Ethanol: ~26 mg/mL (~201.3 mM) Water: ~26 mg/mL (~201.3 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (16.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (16.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 100 mg/mL (774.23 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 7.7417 mL | 38.7087 mL | 77.4174 mL | |
5 mM | 1.5483 mL | 7.7417 mL | 15.4835 mL | |
10 mM | 0.7742 mL | 3.8709 mL | 7.7417 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01529593 | Active Recruiting |
Drug: Temsirolimus Drug: Metformin |
Advanced Cancers | M.D. Anderson Cancer Center | March 26, 2012 | Phase 1 |
NCT04341571 | Active Recruiting |
Dietary Supplement: Probiotics Drug: Metformin |
PreDiabetes Hyperglycemia |
University of Guadalajara | October 24, 2019 | Phase 2 |
NCT05288153 | Active Recruiting |
Drug: Metformin Drug: Folate |
Gastric Intestinal Metaplasia | Xijing Hospital of Digestive Diseases |
April 1, 2022 | Phase 4 |
NCT04055012 | Active Recruiting |
Drug: Metformin Drug: Placebo |
Low Back Pain | Gwendolyn Sowa | January 7, 2020 | Phase 2 |
NCT03031821 | Active Recruiting |
Drug: Metformin Drug: Placebo Oral Tablet |
Prostate Cancer Metabolic Syndrome |
Canadian Urologic Oncology Group | July 12, 2018 | Phase 3 |
Metformin alleviated liver fibrosis via inhibiting the collagen deposition and the activation of hepatic stellate cells. Int Immunopharmacol . 2022 Jul:108:108683. td> |
Metformin induced apoptosis in HSCs to alleviate liver fibrosis. Int Immunopharmacol . 2022 Jul:108:108683. td> |
Metformin reduced mitochondrial membrane potential (ΔΨm) and drove superoxide production in mitochondria. Int Immunopharmacol . 2022 Jul:108:108683. td> |
Metformin induced apoptosis pathway. Int Immunopharmacol . 2022 Jul:108:108683. td> |
Metformin and AICAR downregulate hepatic SREBP-1. J Clin Invest . 2001 Oct;108(8):1167-74. td> |
Metformin inhibits hepatic ACC activity in vivo. J Clin Invest . 2001 Oct;108(8):1167-74. td> |
Metformin mediates AMPK activation in primary hepatocytes. J Clin Invest . 2001 Oct;108(8):1167-74. td> |