Vildagliptin

Description

What is vildagliptin?

Vildagliptin, previously identified as LAF237, is a new oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vidagliptin subsequently acts by inhibiting the inactivation of glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP) by DPP-4.

This inhibitory activity ultimately results in a two-fold action where GLP-1 and GIP are present to potentiate the secretion of insulin by beta cells and suppress glucagon secretion by alpha cells in the islets of Langerhans in the pancreas. It is currently in clinical trials in the U.S. and has been shown to reduce hyperglycemia in type 2 diabetes mellitus. While the drug is still not approved for use in the US, it was approved in Feb 2008 by European Medicines Agency for use within the EU and is listed on the Australian PBS with certain restrictions.

Basic Information

Product Name:	Vildagliptin
Synonyms:	Vildagliptin INN
CAS:	274901-16-5
MF:	C17H25N3O2
MW:	303.4
EINECS:	630-410-0
Product Categories:	Pharmaceutical raw materials; APIs; Circulatory drugs

Chemical Structure

Vildagliptin

Chemical 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
Fp	275.1℃
storage temp.	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

Vildagliptin Uses

Vildagliptin is a selective, competitive and reversible DPP24 inhibitor. Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like polypeptide 21 (GLP21) are important hormones for maintaining glucose concentration in the body, and both have incretin effects. The insulin-promoting effect of GIP in patients with type 2 diabetes is impaired. Only GLP21 can play the role of insulin-stimulating hormone. It promotes insulin secretion by acting on the receptors on the pancreatic β cell membrane. GLP21 can also inhibit the secretion of glucagon and inhibit gastric emptying to increase satiety (suppress appetite). DPP24 binds to protein and exists in many tissues, such as kidney, liver, brush border of small intestine membrane, pancreatic duct, lymphocytes, endothelial cells, and it can be quickly inactivated by hydrolyzing the second alanine at the N-terminal of GLP21 . This product inhibits the activity of the enzyme by combining with DPP24 to form a DPP24 complex. It increases the concentration of GLP21 and promotes the production of insulin by pancreatic β cells, while reducing the concentration of glucagon, thereby reducing blood sugar. And it has no significant effect on body weight.

Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

MSDS: MSDS available.

COA: COA can be available if you send us inquiry.

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