Vildagliptin

(2S)-1-{2-[(3-hydroxyadamantan-1-yl)amino]acetyl}pyrrolidine-2-carbonitrile

Formula: C17H25N3O2 (303.1947)
Chinese Name: 维达列汀
BioDeep ID: BioDeep_00000018146 ( View LC/MS Profile)
SMILES: C1CC(N(C1)C(=O)CNC23CC4CC(C2)CC(C4)(C3)O)C#N



Found 5 Sample Hits

m/z Adducts Species Organ Scanning Sample
304.2023 [M+H]+
PPM:1.2
Homo sapiens esophagus DESI ()
LNTO22_1_4 - MTBLS385
Resolution: 17μm, 82x80

Description

326.1832 [M+Na]+
PPM:2.1
Homo sapiens colorectal adenocarcinoma DESI ()
439TopL, 409TopR, 429BottomL, 419BottomR-profile - MTBLS415
Resolution: 17μm, 157x136

Description

The human colorectal adenocarcinoma sample was excised during a surgical operation performed at the Imperial College Healthcare NHS Trust. The sample and procedures were carried out in accordance with ethical approval (14/EE/0024).

326.1829 [M+Na]+
PPM:3
Homo sapiens NA DESI ()
160TopL,130TopR,150BottomL,140BottomR-profile - MTBLS415
Resolution: 17μm, 142x136

Description

304.2006 [M+H]+
PPM:4.4
Homo sapiens esophagus DESI ()
LNTO22_1_5 - MTBLS385
Resolution: 75μm, 135x94

Description

304.2039 [M+H]+
PPM:6.4
Homo sapiens esophagus DESI ()
LNTO22_1_7 - MTBLS385
Resolution: 75μm, 69x54

Description


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. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucaon release by the alpha cells of 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. A - Alimentary tract and metabolism > A10 - Drugs used in diabetes > A10B - Blood glucose lowering drugs, excl. insulins > A10BH - Dipeptidyl peptidase 4 (dpp-4) inhibitors C78276 - Agent Affecting Digestive System or Metabolism > C29711 - Anti-diabetic Agent > C98086 - Dipeptidyl Peptidase-4 Inhibitor D007004 - Hypoglycemic Agents > D054873 - Dipeptidyl-Peptidase IV Inhibitors D004791 - Enzyme Inhibitors > D011480 - Protease Inhibitors C471 - Enzyme Inhibitor > C783 - Protease Inhibitor Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1].