Vildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity.

Product information

CAS Number: 2133364-01-7

Molecular Weight: 339.43

Formula: C17H29N3O4

Synonym:

LAF237 dihydrate

NVP-LAF 237 dihydrate

Chemical Name: Vildagliptin dihydrate

Smiles: O.O.N#C[C@@H]1CCCN1C(=O)CN[C@]12C[C@]3(O)C[C@H](C1)C[C@H](C2)C3

InChiKey: MVOBUCAQTXEOGS-CGZJGLKQSA-N

InChi: InChI=1S/C17H25N3O2.2H2O/c18-9-14-2-1-3-20(14)15(21)10-19-16-5-12-4-13(6-16)8-17(22,7-12)11-16;;/h12-14,19,22H,1-8,10-11H2;2*1H2/t12-,13+,14-,16+,17-;;/m0../s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. Vildagliptin also promotes cell proliferation.

In Vivo:

Vildagliptin (35 mg/kg; once daily by oral gavage) increases plasma active GLP-1 levels in islets of db/db mice. Vildagliptin (10 µmol/kg; orally) significantly decreases glucose excursions and stimulate insulin secretion in obese male Zucker rats.

References:

1. Cheng Q, et al. Combination of the dipeptidyl peptidase IV inhibitor LAF237 [(S)-1-[(3-hydroxy-1-adamantyl)ammo]acetyl-2-cyanopyrrolidine] with the angiotensin II type 1 receptor antagonist valsartan [N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl]-L-valine] enhances pancreatic islet morphology and function in a mouse model of type 2 diabetes. J Pharmacol Exp Ther. 2008 Dec;327(3):683-91.
2. Shen M, et al. The synergistic effect of valsartan and LAF237 [(S)-1-[(3-hydroxy-1-adamantyl)ammo]acetyl-2-cyanopyrrolidine] on vascular oxidative stress and inflammation in type 2 diabetic mice. Exp Diabetes Res. 2012;2012:146194.
3. Abdelhamid AM, et al. Vildagliptin/Pioglitazone Combination Improved The Overall Glycemic Control In Type I Diabetic Rats. Can J Physiol Pharmacol. 2018 Mar 6. doi: 10.1139/cjpp-2017-0680.

Products are for research use only. Not for human use.