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Vildagliptin

Indications and Usage Mechanisms of Action Adverse reactions
Vildagliptin
Vildagliptin structure
CAS No.
274901-16-5
Chemical Name:
Vildagliptin
Synonyms
Galvus;Laf 237;ZoMelis;Vildaliptin;NVP-LAF 237;Vildgliptin;Vildagliptin;Unii-I6B4B2U96p;Vildagliptin API;Vildagliptin (LAF-237)
CBNumber:
CB71449010
Molecular Formula:
C16H15F6N5O?H3O4P?H2O
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)
Density 
1.27
Flash point:
275.1℃
storage temp. 
-20°C Freezer
CAS DataBase Reference
274901-16-5(CAS DataBase Reference)

SAFETY

Risk Statements  28-38-41-48
Safety Statements  24/25-26-28-36/37/39
RIDADR  3077
HS Code  29339900

Vildagliptin price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 14705 Vildagliptin ≥98% 274901-16-5 10mg $25 2018-11-13 Buy
Cayman Chemical 14705 Vildagliptin ≥98% 274901-16-5 1g $250 2018-11-13 Buy
Cayman Chemical 14705 Vildagliptin ≥98% 274901-16-5 50mg $75 2018-11-13 Buy
Cayman Chemical 14705 Vildagliptin ≥98% 274901-16-5 100mg $113 2018-11-13 Buy

Vildagliptin Chemical Properties,Uses,Production

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( 275)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21935 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1529 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20676 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32452 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070;product@chemlin.com.cn
product@chemlin.com.cn CHINA 3015 60
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24196 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 209 58
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 305 58
Hebei Chisure Biotechnology Co., Ltd.
+8613292890173
0311 66567340 luna@speedgainpharma.com CHINA 1019 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 25796 58

View Lastest Price from Vildagliptin manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-07-17 Vildagliptin
274901-16-5
US $1.00 / Kg/Drum 1KG 99% 9999tons Shandong Kangmailin Chemical Technology Co. Ltd..
2019-07-05 pharma API Vildagliptin
274901-16-5
US $10.00 / KG 1KG 99% 10 mt Hebei Guanlang Biotechnology Co., Ltd.
2018-08-20 Vildagliptin
274901-16-5
US $1.00 / KG 1G 98% 100KG career henan chemical co

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