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Metformin hydrochloride

Oral hypoglycemic agents Adverse effects and precautions Chemical Properties Application Production method
Metformin hydrochloride
Metformin hydrochloride structure
CAS No.
1115-70-4
Chemical Name:
Metformin hydrochloride
Synonyms
big;Medet;DIABEX;meguan;Nelbis;Metrion;diformin;GlucoMet;GlucoMin;GlucoforM
CBNumber:
CB6222671
Molecular Formula:
C4H12ClN5
Formula Weight:
165.62
MOL File:
1115-70-4.mol

Metformin hydrochloride Properties

Melting point:
223-226 °C(lit.)
Flash point:
9℃
storage temp. 
2-8°C
solubility 
Freely soluble in water, slightly soluble in alcohol, practically insoluble in acetone and in methylene chloride
form 
Powder
color 
White
Water Solubility 
Soluble in water (50 mg/ml), ethanol, and DMSO (50 mM).
λmax
233nm(H2O)(lit.)
Merck 
14,5938
InChIKey
OETHQSJEHLVLGH-UHFFFAOYSA-N
CAS DataBase Reference
1115-70-4(CAS DataBase Reference)
FDA UNII
786Z46389E
NCI Dictionary of Cancer Terms
Glucophage; metformin hydrochloride
NCI Drug Dictionary
Glucophage
SAFETY
  • Risk and Safety Statements
Symbol(GHS) 
GHS07,GHS02,GHS06,GHS08
Signal word  Danger
Hazard statements  H225-H301+H311+H331-H370-H302-H315-H319
Precautionary statements  P210-P260-P280-P301+P310-P311-P301+P312+P330-P305+P351+P338-P280a-P301+P312a-P321-P332+P313-P501a
Hazard Codes  Xn,T,F
Risk Statements  22-36/38-39/23/24/25-23/24/25-11
Safety Statements  26-36-45-36/37-16-7
RIDADR  UN1230 - class 3 - PG 2 - Methanol, solution
WGK Germany  3
RTECS  DU1800000
HS Code  29252900
Toxicity LD50 in rats (mg/kg): 1000 orally, 300 s.c. (Rx Bulletin)

Metformin hydrochloride price More Price(62)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich M-072 Metformin hydrochloride solution 1.0?mg/mL in methanol (as free base), ampule of 1?mL, certified reference material, Cerilliant? 1115-70-4 1 mL $103 2021-12-16 Buy
Sigma-Aldrich 317240 Metformin - CAS 1115-70-4 - Calbiochem An antihyperglycemic agent that lowers blood glucose levels without stimulating insulin secretion, promoting weight gain or causing hypoglycemia. 1115-70-4 5 g $119.32 2021-12-16 Buy
Sigma-Aldrich 317240 Metformin 1115-70-4 5gm $124 2021-12-16 Buy
Sigma-Aldrich M0605000 Metformin hydrochloride European Pharmacopoeia (EP) Reference Standard 1115-70-4 $180 2021-12-16 Buy
Sigma-Aldrich BP227 Metformin hydrochloride British Pharmacopoeia (BP) Reference Standard 1115-70-4 $190 2021-12-16 Buy

Metformin hydrochloride Chemical Properties,Uses,Production

Oral hypoglycemic agents

Metformin hydrochloride is a biguanide oral hypoglycemic agent , also known as  Glucophage,  its hypoglycemic effect is weaker than phenformin, the main role is to reduce the glucagon secretion of A cells ,and to promote the conversion of glucose to glycogen, its characteristic effect including that it does not  stimulate pancreatic β-cells to secrete insulin .
The follows are hypoglycemic mechanisms:
1. Increasing the sensitivity of peripheral tissues to insulin, increase insulin-mediated glucose utilization.
2. Increasing glucose utilization of non-insulin-dependent tissues, such as brain, blood cells, kidney medulla, intestine, skin and so on.
3. Inhibiting hepatic gluconeogenesis effect , reducing hepatic glucose output.
4. Inhibiting glucose uptake by intestinal cells.
5. Inhibiting the biosynthesis and storage of cholesterol , lowering blood triglycerides and total cholesterol levels.
Metformin hydrochloride is clinically used for the treatment of type Ⅱ diabetes patients who are not satisfied with simple diet control, especially patients with obesity and hyperinsulinemia, usage of this drug not only displays no hypoglycemic effect, but also there may be weight loss and hyperinsulinemia effect. For some patients with poor efficacy of sulfonylurea ,it may be effective, if it is used with hypoglycemic drugs including sulfonylurea, intestinal glucosidase inhibitors or thiazolidinediones, the results are better than used alone. It can also be used in patients with insulin therapy to reduce the amount of insulin.
At present, domestic manufacturer mainly include the American Shanghai Squibb Pharmaceutical Co., Ltd .

Adverse effects and precautions

Biguanide oral hypoglycemic agents can increase glucose utilization of surrounding tissues and inhibit the intestinal absorption of glucose, and inhibit glycogen gluconeogenesis and hepatic glucose output,it is mainly applied to obesity, dyslipidemia, type II diabetes patients. It almost has no hypoglycemic effect for normal persons ,  2 to 3 hours after taking for diabetes patients ,glucose decreases significantly.
Commonly used oral hypoglycemic agents include phenformin and metformin hydrochloride.
The incidence of adverse effects of metformin hydrochloride is higher than tolbutamide , common gastrointestinal reactions are anorexia, nausea, vomiting, abdominal pain, diarrhea, occasional metallic taste in the mouth, bad breath, nausea, loss of appetite and diarrhea and other gastrointestinal reactions, sometimes  hypoglycemia  is visible  .
Since the biguanide drugs enhance sugar anaerobic glycolysis, and inhibit  glycogen generation, small number of patients may suffer with ketosis or lactic acidosis, which should be particularly vigilant, but metformin effect is weak  , adverse reactions are only  1/50 of other biguanides, and it has rapid clearance, there are no accumulation in the liver, it rarely induces lactic acidosis, sometimes there is mild increase in blood lactate. patients with heart, liver, kidney diseases are prone to these adverse reactions, diabetes patients with these types of complications are hanged. It can reduce the absorption of vitamin B12, but it seldom causes anemia. The following cases are contraindications:
1. Pregnant and lactating women, children under 10 years of age, 80 years of age or older.
2. Diabetic ketoacidosis, diabetic hyperglycemic hyperosmolar syndrome, diabetes lactic acidosis.
3. Severe liver and kidney dysfunction, blood urea nitrogen and creatinine higher than normal, hypovolemic shock, heart failure, AMI, in vivo hypoxic condition such as heart failure, pulmonary insufficiency, or any systemic hypoxia circumstances and other serious heart and lung diseases.
4. Severe infection or trauma, major surgery, clinical hypotension , hypoxia and so on.
5. Complications with severe diabetic nephropathy and retinopathy. When there are symptoms,the drug  should be immediately discontinued; cimetidine can reduce the renal excretion of metformin hydrochloride, agar types can reduce the absorption of metformin, patients must check liver and kidney function and cardiac ketones regularly.
6. Alcoholics, vitamin B12 and folate deficiency which are not corrected.

Chemical Properties

White crystal or crystalline powder. Melting point 232 ℃ (218-220 ℃). Soluble in water, dissolved in methanol, slightly soluble in ethanol, insoluble in ether and chloroform. Odorless, bitter taste.

Application

Production method

After the salifying of dimethylamine and the reaction with dicyandiamide , the product is derived.

Description

Metformin is a biguanide with diverse biological activities. Metformin (250 mg/kg, i.p.) increases hepatic AMPK activity and reduces blood glucose by more than 50% in a liver kinase B1-dependent manner in mice fed normal and high-fat diets, respectively, and reduces blood glucose by 40% in ob/ob mice. It reduces weight gain, hepatic lipid droplet content, and total cholesterol, LDL cholesterol, and triglyceride levels in the plasma of diet-induced obese mice when administered at doses of 10 or 50 mg/kg per day. It also reverses increased hepatic triglyceride and apolipoprotein A5 levels, as well as hepatic steatosis, in a dose-dependent manner in an ob/ob mouse model of non-alcoholic fatty liver disease (NAFLD). Metformin (250 mg/kg) reduces tumor growth in an HCT116 p53-\- human colon cancer mouse xenograft model, but has no effect on HCT116 p53-\- tumors overexpressing recombinant S. cerevisiae Ndi1 NADH dehydrogenase, a single-subunit ortholog of the multi-subunit mammalian mitochondrial complex I. Formulations containing metformin have been used in the treatment of type 2 diabetes.

Chemical Properties

Crystalline Solid

Originator

Diabetex ,Germania

Uses

An oral hypoglycemic agent

Uses

Anti-diabetic and anti-cancer activity

Uses

1,1-Dimethylbiguanide hydrochloride is used as an antidiabetic agent, used in polycystic ovary syndrome, non-alcoholic fatty liver disease and diabetes mellitus type 2. It may also reduce weight gain in people taking atypical antipsychotics, used in a study to investigate its role in enhancing the secretions of plasma active glucagon-like peptide-1 (GLP-1) levels.

Definition

ChEBI: A hydrochloride resulting from the reaction of metformin with one molar equivalent of hydrogen chloride.

Manufacturing Process

The boiling mixture of 1,000 L xylene, 450 kg dimethylamine and 840 kg dicyanamide was added 365 kg hydrogene chloride. Yield of biguanide, 1,1- dimethyl-, hydrochloride 1,588 kg (96%). Biguanide, 1,1-dimethyl-, hydrochloride may be recrystallysed from methanol.

brand name

Fortamet (Andrx); Glucophage (Bristol-Myers Squibb); Glumetza (Depomed); Riomet(Ranbaxy).

Therapeutic Function

Oral hypoglycemic

General Description

1,1-Dimethylbiguanide hydrochloride (metformin) is a strong base. It forms well defined salts and possessing excellent coordination capacity with transition metals, forming highly colored bidentate chelate complexes. Metformin (MET) exists in various forms: diprotonated (H2MET)2+ in strong acidic solution, monoprotonated (HMET)+ in weak acid, MET in neutral and deprotonated (MET)- in strong alkali solution. It is an oral antidiabetic drug. Pharmacokinetics of metformin has been studied. Determination of metformin in human plasma has been described by simple HPLC-UV method. Metformin is reported to increase plasma active glucagon-like peptide-1 (GLP-1) in humans.

Biological Activity

Antidiabetic agent; lowers plasma glucose levels and improves insulin sensitivity. Inhibits hepatic gluconeogenesis via activation of the LKB1/AMPK pathway. Displays antiproliferative effects in cancer cell lines.

Biochem/physiol Actions

Metformin is an antidiabetic agent that reduces blood glucose levels and improves insulin sensitivity. Its metabolic effects, including the inhibition of hepatic gluconeogenesis, are mediated at least in part by activation of the LKB1-AMPK (AMP-activated protein kinase) pathway. Activation of this pathway also appears to be involved in the antiproliferative and proapoptotic actions of metformin in cancer cell lines.

Veterinary Drugs and Treatments

Metformin may be useful in the adjunctive treatment of non-insulin dependent diabetes mellitus in cats. Only limited trials of the drug have been performed in cats, with only very limited success when the drug is used alone. Studies comparing its safety and efficacy with other oral antihyperglycemics (e.g., glipizide or insulin) were not located.

Metformin hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products


Metformin hydrochloride Suppliers

Global( 595)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com China 22607 55
Hubei XinRunde Chemical Co., Ltd.
+8615102730682
02783214688 bruce@xrdchem.cn CHINA 567 55
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 890 55
Hefei TNJ Chemical Industry Co.,Ltd.
+86-0551-65418679
86-0551-65418697 info@tnjchem.com China 3000 55
Shanxi Naipu Import and Export Co.,Ltd
+8613734021967
kaia@neputrading.com CHINA 1011 58
career henan chemical co
+86-0371-55982848
sales@coreychem.com China 29954 58
SHANDONG ZHI SHANG CHEMICAL CO.LTD
+86 18953170293
+86 0531-67809011 sales@sdzschem.com CHINA 2940 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 968 58
Chengdu Biopurify Phytochemicals Ltd.
18482058008 18080483897
maggie@biopurify.com CHINA 2712 58
Hubei Jusheng Technology Co.,Ltd.
86-18871470254
027-59599243 linda@hubeijusheng.com CHINA 28229 58

View Lastest Price from Metformin hydrochloride manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2022-01-19 Metformin Hydrochloride
1115-70-4
US $1.00 / g 1g 99 20tons Shanghai Longyu Biotechnology Co., Ltd.
2022-01-14 Metformin hydrochloride
1115-70-4
US $1.00-499.00 / KG 0.5KG >99% 20tons Anhui Rencheng Technology Co., Ltd
2021-12-01 Metformin Hydrochloride
1115-70-4
US $10.50 / KG 1KG 99% 10 ton Hebei Crovell Biotech Co Ltd

Metformin hydrochloride Spectrum


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