Vildagliptin dihydrate
Vildagliptin dihydrate Basic information
- Product Name:
- Vildagliptin dihydrate
- Synonyms:
-
- Vildagliptin dihydrate
- CAS:
- 2133364-01-7
- MF:
- C17H27N3O3
- MW:
- 321.42
- Mol File:
- 2133364-01-7.mol
Vildagliptin dihydrate Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
Vildagliptin dihydrate Usage And Synthesis
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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