tianfu chem Gliclazide

Details:

Product Name: Gliclazide
Synonyms: )-4-methyl-;1-(3-azabicyclo(3.3.0)oct-3-yl)-3-(p-tolylsulfonyl)urea;1-(hexahydrocyclopenta(c)pyrrol-2(1h)-yl)-3-(p-tolylsulfonyl)-ure;1-(hexahydrocyclopenta(c)pyrrol-2(1h)-yl)-3-(p-tolylsulfonyl)urea;benzenesulfonamide,n-(((hexahydrocyclopenta(c)pyrrol-2(1h)-yl)amino)carbonyl;n-(4-methylbenzenesulfonyl)-n’-(3-azabicyclo(3.3.0)oct-3-yl)urea;s852;se1702
CAS: 21187-98-4
MF: C15H21N3O3S
MW: 323.41
EINECS: 244-260-5
Product Categories: Pharmaceutical;Active Pharmaceutical Ingredients;APIs;Intermediates & Fine Chemicals;Pharmaceuticals;API's;Potassium channel;Aromatics;Sulfur & Selenium Compounds;Other APIs;Pharmaceutical intermediates;Anti diabetic
Mol File: 21187-98-4.mol
Gliclazide Structure
Gliclazide Chemical Properties
Melting point  163-169 °C(lit.)
storage temp.  -20°C Freezer
solubility  methylene chloride: soluble
form  powder
color  white
Merck  14,4439
InChIKey BOVGTQGAOIONJV-UHFFFAOYSA-N
CAS DataBase Reference 21187-98-4(CAS DataBase Reference)
Safety Information
Hazard Codes  Xn,Xi
Risk Statements  21-36/38-46-62-63
Safety Statements  25-26-36/37-53-24/25
RIDADR  3077
WGK Germany  2
RTECS  YT4500000

Gliclazide Usage And Synthesis
Description Gliclazide is an oral antihyperglycemic agent used for the treatment of diabetes mellitus type II. It belongs to the sulfonylurea class of insulin secretagogues, which stimulates β cells of the pancreas to release insulin. Gliclazide binds to the β cell sulfonyl urea receptor (SUR1), further blocking the ATP sensitive potassium channels. Therefore, the potassium efflux substantially decreases, causing depolarization of the β cells. Then the voltage-dependent calcium channels in the β cell are open, resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules. Recent studies have also shown that gliclazide can effectiveimprove anti-oxidant status and nitric oxide-mediated vasodilation in Type 2 diabetes and protect pancreatic beta-cells from damage by hydrogen peroxide.
Hypoglycemic agents Gliclazide, chemical name is 1-(hexahydrocyclopenta [c] pyrrole-2 (1H)-yl)-3-(4-methylphenyl) sulfonyl urea, is the second generation of sulfur ureide oral hypoglycemic agents, and it also has dual function of hypoglycemic and improving blood clotting. It not only can improve the metabolism of diabetic patients, but also can improve or delay the occurrence of diabetic vascular complications. Gliclazide was developed by the French SERVIER company, and listed in France as early as 1972. Its trade names are diamicron gliclazide, methanesulfonic bicyclic urea to g pancreas, methanesulfonic grid urea, glick that sa. It is mainly used for the treatment of the onset of diet and exercise alone control ineffective of adulthood, and no ketosis tendency of light, moderate the type II diabetes. It also can improve diabetic retinopathy and metabolic disorders, vascular function. It can be used with biguanide oral hypoglycemic drugs, and used with insulin to treat insulin-dependent diabetes mellitus, in which condition that insulin dosage can be reduced. 1980s, it began to be supplied into the Chinese market. Now there has been more than 130 countries worldwide that registered and sold.
Pharmacological effects 1. Hypoglycemic effect: gliclazide is the second-generation oral sulfonylurea hypoglycemic agents. Its role is more than ten times stronger than tolbutamide. Mechanism of action is to stimulate pancreatic β cells to release insulin, and then the high blood sugar drops. This may be because that sulfonylurea combines with β cell surface receptor, and increases the activation and simultaneously improves the sensitivity of outer periphery of the target tissue to insulin.
2. It can reduce platelet aggregation and adhesion, and prevent fibrin depositing in the microvasculature.
3. It can lower cholesterol savings, and reduce plasma concentrations of arterial triphosphate glycerides and fatty acids. The role of the three not only can treat diabetes metabolic disorders, but also prevent and treat complications like the development and progression of diabetes-blood vessels, retinal, renal disease.