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Vildagliptin (LAF237 dihydrate; NVP-LAF 237 dihydrate) is a selective dipeptidyl peptidase 4 (DPP4) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. It delays the degradation of glucagon-like peptide-1 (GLP-1). Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity.
ln Vitro |
Vildagliptin inhibits apoptosis to increase β-cell survival. Additionally, vildagliptin stimulates cell division [2].
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ln Vivo |
Vildagliptin raises plasma active GLP-1 levels in the islets of db/db mice when administered orally once daily at a dose of 35 mg/kg [2]. Vildagliptin (10 µmol/kg; oral) in obese male Zucker rats dramatically lowers glucose excursions and increases insulin secretion [1].
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Animal Protocol |
Animal/Disease Models: Male db/db mice (BKS) and wild-type mice [2]
Doses: 35 mg/kg Route of Administration: po (oral gavage); one time/day; for 6 weeks Experimental Results: Increased plasma active GLP-1 levels (22.63±1.19 vs. 11.69±0.44). Animal/Disease Models: Obese male Zucker rat [1] Doses: 10 µmol/kg (pharmacokinetic/PK/PK analysis) Route of Administration: Oral Experimental Results:Dramatically diminished blood sugar fluctuations and stimulated insulin secretion. |
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'-biphen
[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. |
Molecular Formula |
C₁₇H₂₉N₃O₄
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Molecular Weight |
339.43
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CAS # |
2133364-01-7
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Related CAS # |
Vildagliptin;274901-16-5;(2R)-Vildagliptin;1036959-27-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O[C@@]1(C[C@H](C2)C3)C[C@H]3C[C@@]2(NCC(N4CCC[C@H]4C#N)=O)C1.O.O
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Synonyms |
LAF-237 dihydrate NVPLAF 237 dihydrateLAF 237 dihydrate NVP-LAF-237 dihydrateLAF237 dihydrate NVP-LAF 237 dihydrate
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.9461 mL | 14.7306 mL | 29.4612 mL | |
5 mM | 0.5892 mL | 2.9461 mL | 5.8922 mL | |
10 mM | 0.2946 mL | 1.4731 mL | 2.9461 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.