ChemicalBook CAS DataBase List 2133364-01-7

2133364-01-7

Name	Vildagliptin dihydrate
CAS	2133364-01-7
Molecular Formula	C17H27N3O3
Molecular Weight	321.42
MOL File	2133364-01-7.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	Soluble in DMSO

Hazard Information

Uses

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[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 50

DPP-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

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