Vildagliptin dihydrate (LAF237 dihydrate)
(Synonyms: 维格列汀二水合物; LAF237 dihydrate; NVP-LAF 237 dihydrate) 目录号 : GC31492
A DPP-4 inhibitor
Cas No.:2133364-01-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats[3]Rats are randomly divided into four groups. (I) Normal control: Untreated control animals (n=12). (II) Diabetic control: Untreated diabetic group (n=18). (III) Vildagliptin: Diabetic rats treated with Vildagliptin (5 mg/kg) (n=12). (IV) Vildagliptin/Pio: Diabetic rats treated with Vildagliptin (5 mg/kg) and Pio (20 mg/kg) (n=12). Treatments are given once daily per-oral for 7 weeks starting from day 1 of confirmation of diabetes. Blood samples are collected from tail vein weekly for 7 weeks. Animals are sacrificed for further analysis[3].Mice[1]For chronic treatment, 4-week-old obese db/db male mice are randomly assigned to Vildagliptin dosage groups. Each group consists of 6 to 10 mice. The mice receive different concentrations of Vildagliptin dissolved in their drinking water for 8 weeks to determine optimal dose for reducing hyperglycemia and glucose intolerance. From initial pilot studies, the dose of Vildagliptin (1 mg/kg/day) is selected for further analysis. Two additional groups of 4-week-old db/db mice receive either valsartan alone (10 mg/kg/day) or combined with Vildagliptin (1 mg/kg/day)[1]. |
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. | |
Vildagliptin is an inhibitor of dipeptidyl peptidase 4 (DPP-4; Ki = 0.003 ?M).1 It is selective for DPP-4 over DPP-2, DPP-8, and DPP-9 (Kis = >500, 0.81, and 0.095 ?M, respectively). Vildagliptin (3 mg/kg) decreases plasma glucose levels and increases plasma insulin levels during an oral glucose challenge in Zucker fa/fa rats.2 It prevents increases in liver triglyceride and thiobarbituric acid reactive substance (TBARS) levels in a mouse model of non-alcoholic fatty liver disease (NAFLD) induced by a high-cholesterol diet.3 Formulations containing vildagliptin have been used in the treatment of type 2 diabetes.
1.Ikuma, Y., Hochigai, H., Kimura, H., et al.Discovery of 3H-imidazol[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitorsBioorg. Med. Chem.20(19)5864-5883(2012) 2.Burkey, B.F., Li, X., Bolognese, L., et al.Acute and chronic effects of the incretin enhancer vildagliptin in insulin-resistant ratsJ. Pharmacol. Exp. Ther.315(2)688-695(2005) 3.Kamal, S.M.Anti-oxidant and anti-inflammatory effects of vildagliptin in non-alcoholic fatty liver disease of miceInt. J. Med. Nano Res.1(1)1-5(2014)
| Cas No. | 2133364-01-7 | SDF | |
| 别名 | 维格列汀二水合物; LAF237 dihydrate; NVP-LAF 237 dihydrate | ||
| Canonical 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 | ||
| 分子式 | C17H29N3O4 | 分子量 | 339.43 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。