Vildagliptin dihydrate

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Vildagliptin dihydrate Basic information
Product Name:Vildagliptin dihydrate
Synonyms:Vildagliptin dihydrate
CAS:2133364-01-7
MF:C17H27N3O3
MW:321.42
EINECS:
Product Categories:
Mol File:2133364-01-7.mol
Vildagliptin dihydrate Structure
Vildagliptin dihydrate Chemical Properties
storage temp. Store at -20°C
solubility Soluble in DMSO
Safety Information
MSDS Information
Vildagliptin dihydrate Usage And Synthesis
UsesVildagliptin 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[1].
in vivo

Vildagliptin (35 mg/kg; once daily by oral gavage) increases plasma active GLP-1 levels in islets of db/db mice[2].
Vildagliptin (10 μmol/kg; orally) significantly decreases glucose excursions and stimulate insulin secretion in obese male Zucker rats[1].

Animal Model:Male db/db mice (BKS) and wildtype mice[2]
Dosage:35 mg/kg
Administration:Oral gavage; once daily; for 6 weeks
Result:Increased plasma active GLP-1 levels (22.63±1.19 vs. 11.69±0.44).
Animal Model:Obese male Zucker rats[1]
Dosage:10 μmol/kg (Pharmacokinetic Analysis)
Administration:Orally
Result:Significantly decreased glucose excursions and stimulate insulin secretion.
IC 50DPP-4
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. DOI:10.1124/jpet.108.142703
[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. DOI:10.1155/2012/146194
[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. DOI:10.1139/cjpp-2017-0680
Vildagliptin dihydrate Preparation Products And Raw materials
Tag:Vildagliptin dihydrate(2133364-01-7) Related Product Information
(2S)-1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile Vildagliptin Amino Adamantane Impurity 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2R)-2-aMino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1S,3R,5S)- Vildagliptin IMpurity 2 (Mixture of DiastereoMers) Vildagliptin N-Oxide 1-[[[(1-Hydroxymethyl)cyclopentyl]amino]acetyl]-2,5-cis-pyrrolidinedicarbonitrile hydrochloride