Name: Vildagliptin (LAF-237)
Price: 180.00 USD

- Overview
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    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].
    
    [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.
- Properties
  - Alternative Name
    
    (S)-1-(2-(((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)amino)acetyl)pyrrolidine-2-carbonitrile
    
    CAS Number
    
    274901-16-5
    
    Molecular Formula
    
    C17H25N3O2
    
    Molecular Weight
    
    303.4
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥12.05 mg/mL in DMSO; ≥96.4 mg/mL in EtOH with ultrasonic; ≥96.8 mg/mL in H2O with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Yiqian Ren, Yao Qiang, et al. "General Strategy for Bioluminescence Sensing of Peptidase Activity In Vivo Based on Tumor-Targeting Probiotic." Anal Chem. 2021 Mar 9;93(9):4334-4341. PMID:33624497

Vildagliptin (LAF-237)

Vildagliptin (LAF-237)

Background

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