Vildagliptin (LAF-237)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
LAF-237是一种有效的DDP-4抑制剂，IC50值为2.3 nM[1]。
DDP-4是一种表达于大多数种类细胞表面的抗原酶，与信号转导、细胞凋亡和免疫调控相关[1]。
LAF-237是一种特异的DDP4抑制剂，可降低血糖。在对II型糖尿病病人的试验中，LAF-237抑制DPP-4对GLP-1的灭活，使得GLP-1能够增加胰岛素的分泌，减少胰高血糖素释放[2]。
在肥胖雄性Zucker大鼠的葡萄糖耐受实验中，LAF-237可显著减少血糖波动，刺激胰岛素分泌。LAF-237注射后两小时，DDP-4抑制活性达到95%[3]。通过增加beta细胞复制及减少细胞凋亡，LAF-237提高beta细胞数量，并能够在洗脱后维持12天。此外，LAF-237在STZ诱导的糖尿病成年雄性Sprague Dawley大鼠中可保护神经纤维损失[4]。
参考文献：
[1]. Chakraborty S, Rendón-Ramírez A, sgeirsson 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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 303.4 |
| Cas No. | 274901-16-5 |
| Formula | C17H25N3O2 |
| Solubility | ≥12.05 mg/mL in DMSO; ≥96.4 mg/mL in EtOH with ultrasonic; ≥96.8 mg/mL in H2O with ultrasonic |
| Chemical Name | (S)-1-(2-(((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)amino)acetyl)pyrrolidine-2-carbonitrile |
| SDF | Download SDF |
| Canonical SMILES | O[C@@]1(C[C@]2(NCC(N3[C@H](C#N)CCC3)=O)C4)C[C@H](C2)C[C@H]4C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | Vildagliptin是一种有效的DDP-4抑制剂，IC50值为62 nM | |||||
| 靶点 | DDP-4 | |||||
| IC50 | 62 nM | |||||
质量控制和MSDS
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