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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