Vildagliptin (LAF-237)
(Synonyms: 维格列汀; LAF237; NVP-LAF 237) 目录号 : GC16733
A DPP-4 inhibitor
Cas No.:274901-16-5
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
LAF-237 is a potent inhibitor of DDP-4 with IC50 value of 2.3 nM [1].
DDP-4 is an antigenic enzyme expressed on the surface of most cell types and is associated with signal transduction, apoptosis and immune regulation [1].
LAF-237 is a specific inhibitor of DDP4 and can reduce glycemia. When tested on Type II diabetes patients, LAF-237 inhibits the inactivation of GLP-1 by DPP-4, allowing GLP-1 to increase the secretion of insulin and decrease glucagon release [2].
In the glucose tolerance test with obese male Zucker rats, LAF-237 can significantly decrease glucose excursion and stimulates insulin secretion. There are 95% inhibition activities of DDP-4 two hours after the injection of LAF-237[3]. Through enhances beta cell replication and reduces apoptosis, LAF-237 increases in the number of beta cell and can sustain for 12 days after washout LAF-237. Also, LAF-237 can protect nerve fiber loss in STZ-induced diabetic adult male Sprague Dawley rats [4].
References:
[1]. Chakraborty S, Rendón-Ramírez A, Ásgeirsson B, et al. The dipeptidyl peptidase IV inhibitors vildagliptin and K-579 inhibit a phospholipase C: a case of promiscuous scaffolds in proteins. F1000Res, 2013, 2: 286.
[2]. Ahrén B, Landin-Olsson M, Jansson PA, et al. Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes. The Journal of Clinical Endocrinology and Metabolism, 2004, 89 (5): 2078–84.
[3] Villhauer EB, et al. 1-[[(3-hydroxy-1-adamantyl) amino] acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. J Med Chem, 2003, 46(13), 2774-2789.
[4] Duttaroy A, et al. Combination therapy with nateglinide and vildagliptin improves postprandial metabolic derangements in Zucker fatty rats. Eur J Pharmacol, 2011, 650(2-3), 703-707.
| Cas No. | 274901-16-5 | SDF | |
| 别名 | 维格列汀; LAF237; NVP-LAF 237 | ||
| 化学名 | (2S)-1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile | ||
| Canonical SMILES | C1CC(N(C1)C(=O)CNC23CC4CC(C2)CC(C4)(C3)O)C#N | ||
| 分子式 | C17H25N3O2 | 分子量 | 303.4 |
| 溶解度 | ≥ 12.05 mg/mL in DMSO, ≥ 96.4 mg/mL in EtOH with ultrasonic, ≥ 96.8 mg/mL in Water with ultrasonic | 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 | 3.296 mL | 16.4799 mL | 32.9598 mL |
| 5 mM | 0.6592 mL | 3.296 mL | 6.592 mL |
| 10 mM | 0.3296 mL | 1.648 mL | 3.296 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。