ChemicalBook
Chinese Japanese Germany Korea

Vildagliptin

Uses Indications and Usage Mechanisms of Action Adverse reactions
Vildagliptin
Vildagliptin structure
CAS No.
274901-16-5
Chemical Name:
Vildagliptin
Synonyms
dagL;Galvus;Laf 237;ZoMelis;DSP7238;Vigliptin;NVP-LAF 237;Vildgliptin;Vildaliptin;Vildagliptin
CBNumber:
CB71449010
Molecular Formula:
C17H25N3O2
Formula Weight:
303.4
MOL File:
274901-16-5.mol

Vildagliptin Properties

Melting point:
153-155?C
alpha 
-78.3° (c = 9.73 in methanol)
Boiling point:
531.3±50.0 °C(Predicted)
Density 
1.27
Flash point:
275.1℃
storage temp. 
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
pka
15.05±0.40(Predicted)
CAS DataBase Reference
274901-16-5(CAS DataBase Reference)
FDA UNII
I6B4B2U96P
NCI Drug Dictionary
vildagliptin
ATC code
A10BH02
SAFETY
  • Risk and Safety Statements
Risk Statements  28-38-41-48
Safety Statements  24/25-26-28-36/37/39
RIDADR  3077
HS Code  29339900

Vildagliptin price More Price(43)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 14705 Vildagliptin ≥98% 274901-16-5 10mg $25 2021-12-16 Buy
Cayman Chemical 14705 Vildagliptin ≥98% 274901-16-5 1g $250 2021-12-16 Buy
TRC V305000 Vildagliptin 274901-16-5 1g $290 2021-12-16 Buy
TRC V305000 Vildagliptin 274901-16-5 50mg $150 2021-12-16 Buy
Usbiological 291956 Vildagliptin 274901-16-5 50mg $319 2021-12-16 Buy

Vildagliptin Chemical Properties,Uses,Production

Uses

Glyptins are class of oral anti-hyperglycemic agents that inhibit dipeptidyl peptidase 4 (DPP-4), which can act as a serine exopeptidase. Aside from their use in type 2 diabetes, gliptins have positive cardiovascular and anti-inflammtatory effects. Antidiabetic.

Indications and Usage

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.

Mechanisms of Action

Vildagliptin is a selective, competitive and reversible DPP-4 inhibitor. Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 21 (GLP21) are important hormones that regulate body glucose concentration and have the same functions as intestinal insulin. Type-2 diabetes patients suffer from GIP insulin secretion failure, so only their GLP21 can promote insulin secretion by affecting receptors on islet beta cell membranes. GLP21 can also inhibit glucagon secretion and inhibit gastric clearing to extend the feeling of fullness (control appetite). DPP-4 binds with proteins in many types of tissues, including tissue in the kidney, liver, small intestine brush border, pancreatic duct, lymph cells, and endothelial cells, and it can deactivate GLP21 by hydrolyzing its N-terminal position-2 alanine. Vildagliptin binds with DPP-4 to produce a DPP-4 compound and inhibit its activity. It increases GLP21 concentration and promotes islet beta cells to produce insulin, while also lowering glucagon concentration, thus lowering blood sugar. Vildagliptin has not noticeable effects on weight.

Adverse reactions

Most common adverse reactions include headache, nasopharyngitis, coughing, constipation, dizziness and excess sweating. There have been very rare cases of hypotension, but it is unclear if conditions are related to this drug. Almost all research shows that the hypoglycemia occurrence rate while using Vildagliptin is similar to the rate when using a placebo. Control trials showed that compared to thiazolidinediones, Vildagliptin causes a similar occurrence rate of headaches, rashes, and other adverse reactions, but Vildagliptin has a lower occurrence rate of adverse reactions forcing patients to cease treatment and of severe adverse reactions.

Description

Vildagliptin, a DPP-4 inhibitor, was launched for the oral treatment of type 2 diabetes. Vildagliptin is the second DPP-4 inhibitor to reach the market behind sitagliptin, which was introduced in 2006. DPP-4 inhibitors act by slowing the inactivation of incretins, which are endogenous peptides involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase the synthesis and release of insulin from pancreatic βcells via intracellular signaling pathways involving cAMP. GLP-1 also lowers glucagon secretion from pancreatic α cells, which leads to reduced hepatic glucose production. However, although GLP-1 and GIP effectively lower blood glucose, they are short-lived as a result of rapid inactivation by the ubiquitous serine protease DPP-4. By inhibiting DPP-4, vildagliptin increases the concentration and duration of active incretin levels, which in turn results in increased insulin release and decreased glucagon levels in a glucose-dependent manner. Both vildagliptin and sitagliptin are potent, competitive, reversible inhibitors of DPP- 4 (IC50=3.5 and 18 nM, respectively), and they both show slow, tight-binding inhibition kinetics.

Chemical Properties

White Solid

Originator

Novartis (US)

Uses

Vildagliptin (LAF-237) inhibits DPP?4 with IC50 of 2.3 nM

Uses

The major metabolite of Vildagliptin

Uses

Labelled Vildagliptin. It is a new oral anti-hyperglycemic agent of a new dipeptidyl peptidase-IV (DPP-IV) inhibitor class of drugs. Antidiabetic.

Uses

A metabolite of Vildagliptin

brand name

Galvus

Side effects

The most common adverse events reported in patients receiving vildagliptin included headache, nasopharyngitis, cough, constipation, dizziness, and increased sweating. Vildagliptin is not recommended for patients with liver impairment.

Chemical Synthesis

Vildagliptin is chemically derived in three steps starting from L-prolinamide via acylation with chloroacetyl chloride to produce 1-(chloroacetyl)-L-prolinamide, subsequent dehydration of the carboxamide group to the nitrile with trifluoroacetic anhydride, and condensation of the 1-(chloroacetyl)-L-prolinenitrile intermediate with 3-hydroxyadamantan-1-amine.

Vildagliptin Preparation Products And Raw materials

Raw materials

Preparation Products


Vildagliptin Suppliers

Global( 418)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Echemi Group
18905328650 86-18905328650
pharma@echemi.com CHINA 215 58
Henan DaKen Chemical CO.,LTD.
+86-371-66670886
info@dakenchem.com China 15427 58
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com China 22607 55
Shanghai Time Chemicals CO., Ltd.
+8618017249410 +86-021-57951555
+86-021-57951555 jack.li@time-chemicals.com China 1807 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 9134 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070
product@chemlin.com.cn CHINA 3013 60
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26782 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 341 58
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 296 58

View Lastest Price from Vildagliptin manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2022-01-20 Top quality API Vildagliptin with best price
274901-16-5
US $1.00 / KG 1KG 99% 20tons Shanxi Naipu Import and Export Co.,Ltd
2022-01-20 pharma API cas 274901-16-5 Vildagliptin
274901-16-5
US $1.00 / KG 1KG 99% 20tons Shanxi Naipu Import and Export Co.,Ltd
2022-01-07 Vildagliptin
274901-16-5
US $300.00 / KG 10g 99% 500kg/month HEBEI YINGONG NEW MATERIAL TECHNOLOGY CO.,LTD

274901-16-5(Vildagliptin)Related Search:


Copyright 2017 © ChemicalBook. All rights reserved