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Purity: ≥98%
Metformin HCl is a hypoglycemic medication used in the treatment of type 2 diabetes (non-insulin-dependent diabetes mellitus). It decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin 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.
| Targets |
AMPK; Autophagy; Mitophagy
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| ln Vitro |
The proliferation of ESCs is inhibited by metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride) in a concentration-dependent manner. For A-ESCs, the IC50 is 2.45 mM, and for N-ESCs, it is 7.87 mM. Compared to cells in the proliferative phase, metformin has a more noticeable effect on AMPK signaling activity in A-ESCs from the secretory phase[2]. In cultured rat hepatocytes, metformin hydrochloride (0-500 μM) reduces glycogen production in a dose-dependent manner, with an IC50 value of 196.5 μM[3]. With an IC50 of 5 mM, metformin hydrochloride exhibits both cytotoxic and viable effects on PC-3 cells[4].
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| ln Vivo |
Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride; 100 mg/kg, po) alone, and metformin (25, 50, 100 mg/kg) with NSC 37745 groups attenuates myocyte necrosis through histological analysis[1].
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| Cell Assay |
ESCs are plated in 96-well plates at a concentration of 1×103cells/well. After attachment, cells are treated with different doses of metformin/compound C for 0 min, 15 min, 1 h, and 24 h. MTT assays are performed as described previously. In brief, MTT (5 mg/mL) is added to the 96-well plates at a volume of 10 μL/well, and the plates are incubated for 4 h. The MTT reaction is terminated by removal of the culture medium containing MTT, and 100 μL DMSO per well are added and incubated at RT on a shaker for 10 min to ensure that the crystals had dissolved sufficiently. Absorbance values are measured at 595 nm. Cell proliferation (percentage of control) is calculated as follows: absorbance (experimental group)/absorbance (control group). Cell proliferation inhibition (percentage of control) is calculated as follows: 100%−cell proliferation (percentage of control). Each experiment is performed in duplicate and repeated six times to assess result consistency [2].
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| Animal Protocol |
The animals are randomized into six groups consisting of six rats each. Rats in group 1 (control) receives a subcutaneous injection of physiological saline (0.5 mL) and are left untreated for the entire experimental period. Rats in group 2 receives an oral administration of metformin (100 mg/kg; twice daily) for 2 days and are subcutaneously injected with saline at an interval of 24 h for 2 consecutive days. Rats in group 3 (MI control) receives an oral administration of saline (twice daily) for 2 days and are sc injected with isoproterenol (100 mg/kg) daily for 2 consecutive days at an interval of 24 h. Rats in groups 4 to 6 are treated with metformin at 25, 50, and 100 mg/kg. Metformin is dissolved in saline and is gavaged at a volume of 0.25-0.5 mL twice a day at an interval of 12 h, started immediately before isoproterenol injection [1].
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| References |
[1]. Soraya H, et al. Acute treatment with metformin improves cardiac function following NSC 37745 induced myocardial infarction in rats. Pharmacol Rep. 2012;64(6):1476-84.
[2]. Xue J, et al. Metformin inhibits growth of eutopic stromal cells from adenomyotic endometrium via AMPK activation and subsequent inhibition of AKT phosphorylation: a possible role in the treatment of adenomyosis. Reproduction. 2013 Aug 21;146(4):397-406. [3]. Otto M, et al. Metformin inhibits glycogen synthesis and gluconeogenesis in cultured rat hepatocytes. Diabetes Obes Metab. 2003 May;5(3):189-94. [4]. Avci CB, et al. Therapeutic potential of an anti-diabetic drug, metformin: alteration of miRNA expression in prostate cancer cells. Asian Pac J Cancer Prev. 2013;14(2):765-8 |
| Molecular Formula |
C4H11N5.HCL
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| Molecular Weight |
165.62
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| Exact Mass |
165.0781
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| Elemental Analysis |
C, 29.01; H, 7.30; Cl, 21.40; N, 42.29
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| CAS # |
1115-70-4
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| Related CAS # |
Metformin-d6 hydrochloride;1185166-01-1; 657-24-9; 1115-70-4 (HCl); 121369-64-0 (glycinate); 58840-24-7 (orotate); 34461-22-8 ( embonate); 1384526-74-2 (icosapent)
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| Appearance |
White to off-white solid
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| LogP |
1.06
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| tPSA |
88.990
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| SMILES |
N(/C(=N\[H])/N=C(\N([H])[H])/N([H])[H])(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
OETHQSJEHLVLGH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C4H11N5.ClH/c1-9(2)4(7)8-3(5)6;/h1-2H3,(H5,5,6,7,8);1H
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| Chemical Name |
1,1-Dimethylbiguanide hydrochloride
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| Synonyms |
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (18.11 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (18.11 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 (603.79 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 | 6.0379 mL | 30.1896 mL | 60.3792 mL | |
| 5 mM | 1.2076 mL | 6.0379 mL | 12.0758 mL | |
| 10 mM | 0.6038 mL | 3.0190 mL | 6.0379 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.
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