Product Name: Vildagliptin (LAF-237)
CAS No.: 274901-16-5
Information: DPP-4 inhibitor.
Description: Vildagliptin is a potent inhibitor of DDP-4 with IC50 value of 62 nM.
Other Names: LAF-237
Chemical Name (2S)-1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile
Canonical SMILES:C1CC(N(C1)C(=O)CNC23CC4CC(C2)CC(C4)(C3)O)C#N
MF: C17H25N3O2
MW: 303.40
Purity: 99%
Type: Treatment of diabetes Agents
Grade Standard: Medicine Grade
Model Number: API-Vidagliptin
Brand Name: Huavet
Place of Origin: Shaanxi, China (Mainland)
Solubility: Soluble in DMSO > 10 mM
Storage: Store at -20°C
General tips: For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition: Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request.
Background: LAF-237 is a potent inhibitor of DDP-4 with IC50 value of 2.3 nM [1].
DDP-4 is an antigenic enzyme expressed on the surface of most cell types and is associated with signal transduction, apoptosis and immune regulation [1].
LAF-237 is a specific inhibitor of DDP4 and can reduce glycemia. When tested on Type II diabetes patients, LAF-237 inhibits the inactivation of GLP-1 by DPP-4, allowing GLP-1 to increase the secretion of insulin and decrease glucagon release [2].
In the glucose tolerance test with obese male Zucker rats, LAF-237 can significantly decrease glucose excursion and stimulates insulin secretion. There are 95% inhibition activities of DDP-4 two hours after the injection of LAF-237[3]. Through enhances beta cell replication and reduces apoptosis, LAF-237 increases in the number of beta cell and can sustain for 12 days after washout LAF-237. Also, LAF-237 can protect nerve fiber loss in STZ-induced diabetic adult male Sprague Dawley rats [4].
References:
[1]. Chakraborty S, Rendón-Ramírez A, Ásgeirsson B, et al. The dipeptidyl peptidase IV inhibitors vildagliptin and K-579 inhibit a phospholipase C: a case of promiscuous scaffolds in proteins. F1000Res, 2013, 2: 286.
[2]. Ahrén B, Landin-Olsson M, Jansson PA, et al. Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes. The Journal of Clinical Endocrinology and Metabolism, 2004, 89 (5): 2078–84.
[3] Villhauer EB, et al. 1-[[(3-hydroxy-1-adamantyl) amino] acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. J Med Chem, 2003, 46(13), 2774-2789.
[4] Duttaroy A, et al. Combination therapy with nateglinide and vildagliptin improves postprandial metabolic derangements in Zucker fatty rats. Eur J Pharmacol, 2011, 650(2-3), 703-707.
Usage: Pharmaceutical Intermediates
Inventory status: in stock
Shelf life: 2 years
Sample: Available
COA (Certificate of Analysis): Available
MSDS (Material Safety Data Sheet): Available
HPLC Spectrum: Available
ISO: Approved
GC: Available
NMR (Nuclear Magnetic Resonance): Available
Packaging Details: 1g, 5g, 10g, 50g,100g/bottle, 1kg/tin for trial order,25kg/drum for commercial quantity. Specific packing required by customer
Delivery Detail: Prompt shipment
Related Antibodies:
*DPP4 Antibody (89F4)
*DPP4 Antibody (68R3)
*DPP4 Antibody (46I2)
*DPP4 Antibody
