274901-16-5 C16H1...

274901-16-5 C16H15F6N5O?H3O4P?H2O Vildagliptin
274901-16-5 C16H15F6N5O?H3O4P?H2O Vildagliptin
274901-16-5 C16H15F6N5O?H3O4P?H2O Vildagliptin
274901-16-5 C16H15F6N5O?H3O4P?H2O Vildagliptin
274901-16-5 C16H15F6N5O?H3O4P?H2O Vildagliptin

274901-16-5 C16H15F6N5O?H3O4P?H2O Vildagliptin

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10 Gram

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  • Min.Order :10 Gram
  • Purity: 99%
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274901-16-5 C16H15F6N5O?H3O4P?H2O Vildagliptin 274901-16-5 C16H15F6N5O?H3O4P?H2O

Quick Details

  • Appearance:white powder
  • Application:Labelled Vildagliptin. It is a new oral anti-hyperglycemic agent of a new dipeptidyl peptidase-IV (DPP-IV) inhibitor class of drugs. Antidiabetic.
  • PackAge:Woven bag
  • ProductionCapacity:1|Kilogram|Day
  • Storage:Normal temperature
  • Transportation:Ocean shipping Express delivery

Superiority:

Vildagliptin Basic information
Treatment of type 2 diabetes drugs Pharmacological effects Production method Adverse reactions
Product Name: Vildagliptin
Synonyms: Vildagliptin (NVP-LAF 237);(-)-(2S)-1-[[(3-Hydroxytricyclo[3.3.1.1[3,7]]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile;Vildagliptin;(-)-(2S)-1-[[(3-Hydroxytricyclo[3.3.1.1[3,7]]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile;2-Pyrrolidinecarbonitrile, 1-(((3-hydroxytricyclo(3.3.1.13,7)dec-1-yl)amino)acetyl)-, (2S)-;Galvus;Laf 237;Unii-I6B4B2U96p
CAS: 274901-16-5
MF: C16H15F6N5O H3O4P H2O
MW: 303.4
EINECS:  
Product Categories: Amines;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Isotope Labelled Compounds;Metabolites & Impurities;API;Inhibitor;Galvus;Other APIs
Mol File: 274901-16-5.mol
Vildagliptin Structure
 
Vildagliptin Chemical Properties
mp  153-155 C
storage temp.  -20°C Freezer
CAS DataBase Reference 274901-16-5(CAS DataBase Reference)
 
Safety Information
MSDS Information
 
 
Vildagliptin Usage And Synthesis
Treatment of type 2 diabetes drugs Vildagliptin (vildagliptin), developed by Novartis (Novartis) Pharmaceutical Co., Ltd, is another oral administrated inhibitor of Dipeptidyl peptidase-IV after sitagliptin (sitagliptin). In 2008, it is approved for marketing in the European Union for the treatment of type 2 diabetes.
Diabetes is a chronic metabolic disease with its prevalence being increased year by year. Type 2 diabetes is a complicated diseases caused with the combined action between polygenic genetic factors and environmental factors.
Dipeptidyl peptidase IV (DPP-IV) inhibitors are a new class of anti-diabetic drugs which induces and facilitate the biosynthesis and secretion of insulin. It plays a role in lowering the blood carbohydrate concentration through multiple mechanisms such as inhibiting the β cell apoptosis, inhibiting glucagon secretion and reducing food intake. During its lowering effect on reducing blood carbohydrate levels, it can also reverse the situation of deteriorating function of pancreas islet for diabetic patients at the same time. Vildagliptin is the representative of drugs among the dipeptidyl peptidase inhibitor. It exhibited a good anti-diabetic effects and tolerance no matter whether it is being administered alone or in combination with metformin and insulin medication in clinical studies.
Pharmacological effects Vildagliptin is a selective, competitive and reversible inhibitor of DPP24. Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 21 (GLP21) are both essential hormones in maintaining the in vivo glucose concentrations which both have incretin effect. Insulin secretion effect of GIP in patients of type 2 diabetes GIP is destroyed with only GLP21 plays a function of insulinotropin secretion. GLP21 promotes the secretion of insulin by acting on pancreatic β cell membrane receptors. GLP21 can also inhibit the glucagon secretion and inhibit the gastric emptying thereby increasing satiety (appetite suppressant). DPP24 binds to protein and is presented in many tissues, such as brush-like kidney, liver, small intestine edges of the membrane, the pancreatic duct cells, and endothelial cells. DPP24 can rapidly deactivate GLP21 by hydrolysis the first two N-terminal alanine of GLP21. This product can form complex with DPP24 to inhibit the enzyme activity. At the same time of improving concentration of GLP21 and promoting pancreatic β cells to produce insulin, it reduces the glucagon concentrations, thereby reducing blood sugar with no significant effect on body weight.
Production method L-proline has its amino group protected by di-tert-butyl dicarbonate ester, and further goes through carbonylamino reaction together with ammonia at the presence of 1- (3-dimethylaminopropyl) -3-ethyl carbodiimide (EDC). Then remove the Boc protecting group with hydrochloric acid to obtain L- prolinamide (intermediate 4), L-prolinamide is further acylated by chloroacetyl chloride to obtain (S)-N-chloroacetyl-2-carbamoyl-pyrrolidin alkoxy (intermediate 2); dehydrate to obtain (S) -N- chloroacetyl-2-cyano pyrrolidine (intermediate 3), and finally have nucleophilic reaction with 3-amino-1-adamantanol (4) to obtain vildagliptin.
L- prolinamide prepared vildagliptin chemical reaction scheme
Figure 1 L- prolinamide prepared vildagliptin chemical reaction scheme
The above information is edited by the Chemicalbook of Dai Xiongfeng.
Adverse reactions 1. The most common adverse reactions include headache, nasopharyngitis, cough, constipation, dizziness and sweating. Very small number of patients got hypertension medication symptoms, but the correlation with the drug is still not clear. Almost all of the research results have confirmed that the use of incidence of hypoglycemia upon using vildagliptin is approximate to that upon using placebo.
2. Control trial has found that compared with thiazolidinediones, the incidence of adverse reactions in patients such as headache, rash is similar while using vildagliptin. However, the incidence of stopping drug due to adverse reactions or severe adverse reactions is the lowest when using vildagliptin.
Chemical Properties White Solid
Usage Vildagliptin (LAF-237) inhibits DPP 4 with IC50 of 2.3 nM
Usage The major metabolite of Vildagliptin
Usage Labelled Vildagliptin. It is a new oral anti-hyperglycemic agent of a new dipeptidyl peptidase-IV (DPP-IV) inhibitor class of drugs. Antidiabetic.
Usage A metabolite of Vildagliptin
 
Vildagliptin Preparation Products And Raw materials
 

 

Details:

Vildagliptin Basic information
Treatment of type 2 diabetes drugs Pharmacological effects Production method Adverse reactions
Product Name: Vildagliptin
Synonyms: Vildagliptin (NVP-LAF 237);(-)-(2S)-1-[[(3-Hydroxytricyclo[3.3.1.1[3,7]]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile;Vildagliptin;(-)-(2S)-1-[[(3-Hydroxytricyclo[3.3.1.1[3,7]]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile;2-Pyrrolidinecarbonitrile, 1-(((3-hydroxytricyclo(3.3.1.13,7)dec-1-yl)amino)acetyl)-, (2S)-;Galvus;Laf 237;Unii-I6B4B2U96p
CAS: 274901-16-5
MF: C16H15F6N5O H3O4P H2O
MW: 303.4
EINECS:  
Product Categories: Amines;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Isotope Labelled Compounds;Metabolites & Impurities;API;Inhibitor;Galvus;Other APIs
Mol File: 274901-16-5.mol
Vildagliptin Structure
 
Vildagliptin Chemical Properties
mp  153-155 C
storage temp.  -20°C Freezer
CAS DataBase Reference 274901-16-5(CAS DataBase Reference)
 
Safety Information
MSDS Information
 
 
Vildagliptin Usage And Synthesis
Treatment of type 2 diabetes drugs Vildagliptin (vildagliptin), developed by Novartis (Novartis) Pharmaceutical Co., Ltd, is another oral administrated inhibitor of Dipeptidyl peptidase-IV after sitagliptin (sitagliptin). In 2008, it is approved for marketing in the European Union for the treatment of type 2 diabetes.
Diabetes is a chronic metabolic disease with its prevalence being increased year by year. Type 2 diabetes is a complicated diseases caused with the combined action between polygenic genetic factors and environmental factors.
Dipeptidyl peptidase IV (DPP-IV) inhibitors are a new class of anti-diabetic drugs which induces and facilitate the biosynthesis and secretion of insulin. It plays a role in lowering the blood carbohydrate concentration through multiple mechanisms such as inhibiting the β cell apoptosis, inhibiting glucagon secretion and reducing food intake. During its lowering effect on reducing blood carbohydrate levels, it can also reverse the situation of deteriorating function of pancreas islet for diabetic patients at the same time. Vildagliptin is the representative of drugs among the dipeptidyl peptidase inhibitor. It exhibited a good anti-diabetic effects and tolerance no matter whether it is being administered alone or in combination with metformin and insulin medication in clinical studies.
Pharmacological effects Vildagliptin is a selective, competitive and reversible inhibitor of DPP24. Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 21 (GLP21) are both essential hormones in maintaining the in vivo glucose concentrations which both have incretin effect. Insulin secretion effect of GIP in patients of type 2 diabetes GIP is destroyed with only GLP21 plays a function of insulinotropin secretion. GLP21 promotes the secretion of insulin by acting on pancreatic β cell membrane receptors. GLP21 can also inhibit the glucagon secretion and inhibit the gastric emptying thereby increasing satiety (appetite suppressant). DPP24 binds to protein and is presented in many tissues, such as brush-like kidney, liver, small intestine edges of the membrane, the pancreatic duct cells, and endothelial cells. DPP24 can rapidly deactivate GLP21 by hydrolysis the first two N-terminal alanine of GLP21. This product can form complex with DPP24 to inhibit the enzyme activity. At the same time of improving concentration of GLP21 and promoting pancreatic β cells to produce insulin, it reduces the glucagon concentrations, thereby reducing blood sugar with no significant effect on body weight.
Production method L-proline has its amino group protected by di-tert-butyl dicarbonate ester, and further goes through carbonylamino reaction together with ammonia at the presence of 1- (3-dimethylaminopropyl) -3-ethyl carbodiimide (EDC). Then remove the Boc protecting group with hydrochloric acid to obtain L- prolinamide (intermediate 4), L-prolinamide is further acylated by chloroacetyl chloride to obtain (S)-N-chloroacetyl-2-carbamoyl-pyrrolidin alkoxy (intermediate 2); dehydrate to obtain (S) -N- chloroacetyl-2-cyano pyrrolidine (intermediate 3), and finally have nucleophilic reaction with 3-amino-1-adamantanol (4) to obtain vildagliptin.
L- prolinamide prepared vildagliptin chemical reaction scheme
Figure 1 L- prolinamide prepared vildagliptin chemical reaction scheme
The above information is edited by the Chemicalbook of Dai Xiongfeng.
Adverse reactions 1. The most common adverse reactions include headache, nasopharyngitis, cough, constipation, dizziness and sweating. Very small number of patients got hypertension medication symptoms, but the correlation with the drug is still not clear. Almost all of the research results have confirmed that the use of incidence of hypoglycemia upon using vildagliptin is approximate to that upon using placebo.
2. Control trial has found that compared with thiazolidinediones, the incidence of adverse reactions in patients such as headache, rash is similar while using vildagliptin. However, the incidence of stopping drug due to adverse reactions or severe adverse reactions is the lowest when using vildagliptin.
Chemical Properties White Solid
Usage Vildagliptin (LAF-237) inhibits DPP 4 with IC50 of 2.3 nM
Usage The major metabolite of Vildagliptin
Usage Labelled Vildagliptin. It is a new oral anti-hyperglycemic agent of a new dipeptidyl peptidase-IV (DPP-IV) inhibitor class of drugs. Antidiabetic.
Usage A metabolite of Vildagliptin
 
Vildagliptin Preparation Products And Raw materials
 
   HenNan sunlake enterprise corporation is located in Henan Province , The central plain of China , Which enjoys favorable geogeaphical position and convenient transportion, The com[any was established in june. 1998 , until now having more than 18 years experience in manufacturing & exporting chemical raw material . 
   Sunlake is a professional manufacturer engaged in producing and selling chemicals,including Organic & inorganic chemicals , pigments & Dyestuffs , Water treatment chemicals , Food & FEED additives and others . these products have been being well exported to europe , southeast Asia , the Middle East , Africa , South America and some other countries and areas. 
    We sincerely welcome foreign friends to visit our plant for cooperation. With the idea of "quality first,credit priority, Excellent service", We are highly acknowledged by customers for good quality and competitive price. More importantly , the company has a strong R & D team, who are professional engineers and scholars with Ph. D. .So we are confident to serve you better with our high - quality products and professional team. 
     We are taking great efforts to provide our customers with demanded goods and professional services, and continuously improve our core ability of competition and get the momentum for sustainable development, and finally make us being a reliable and professional wupplier in international market. We welcome any serious inquiries from all customers of the world, and sincerely hope to cooperate with you for a brilliant future!
 

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