NVP DPP 728 dihydrochloride
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.
Ki值:抑制人DPP-IV酰胺水解活性,Ki值为11 nM[1]
二肽基肽酶4又被称为DPP-4或gliptins,其抑制剂是一类口服降糖药,可用于治疗II型糖尿病。NVP DPP 728 dihydrochloride是二肽基肽酶(DPP)-IV的强效的口服活性抑制剂。
体外实验:NVP-DPP728可以抑制人的DPP-IV酰胺分解活性,Ki值为11 nM,kon值为1.3×105 /M/s,koff为1.3×10/s。NVP-DPP728以两步法抑制机制抑制DPP-IV的活性。总之,这些数据表明,NVP-DPP728通过形成一种新型的、可逆的过渡态特性的腈依赖性复合体,抑制DPP-IV的活性[1]。
在体实验:在老年的Wistar 或DPP-IV(+) F344大鼠中,与年轻的对照组相比,口服葡萄糖后,衰老引起早期胰岛素反应降低,而在老年的DPP-IV(-) F344大鼠中没有这种现象。口服葡萄糖后,老年DPP-IV(-) F344大鼠比老年DPP-IV(+) F344和Wistar大鼠有更好的葡萄糖耐受性,这与早期胰岛素响应的维持相关。在老年DPP-IV(+) Wistar 和F344大鼠中,口服葡萄糖后,NVP-DPP728抑制血浆中DPP-IV活性,增强早期的胰岛素响应,最终提高葡萄糖耐受性。相比之下,在老年的DPP-IV(-) F344大鼠中,口服葡萄糖后,NVP-DPP728不影响葡萄糖的耐受性,这些研究结果表明,在老年大鼠中,NVP-DPP728直接抑制血浆DPP-IV的活性,随后增加内源性肠促胰岛素的作用,最终改善葡萄糖的耐受性[2]。
临床试验:NVP-DPP728目前正处于临床前开发阶段,没有正在进行的临床试验。
参考文献:
[1] Hughes TE, Mone MD, Russell ME, Weldon SC, Villhauer EB. NVP-DPP728 (1-[[[2-[(5-cyanopyridin-2-yl)amino]ethyl]amino]acetyl]-2-cyano-(S)-pyrrolidine), a slow-binding inhibitor of dipeptidyl peptidase IV. Biochemistry. 1999;38(36):11597-603.
[2] Mitani H, Takimoto M, Kimura M. Dipeptidyl peptidase IV inhibitor NVP-DPP728 ameliorates early insulin response and glucose tolerance in aged rats but not in aged Fischer 344 rats lacking its enzyme activity. Jpn J Pharmacol. 2002;88(4):451-8.
Physical Appearance | A yellow oil |
Storage | Desiccate at RT |
M.Wt | 371.27 |
Cas No. | 247016-69-9 |
Formula | C15H18N6O·2HCl |
Solubility | ≥17.75 mg/mL in DMSO with gentle warming; ≥81 mg/mL in EtOH; ≥82 mg/mL in H2O |
Chemical Name | 6-[2-[[2-(2-cyanopyrrolidin-1-yl)-2-oxoethyl]amino]ethylamino]pyridine-3-carbonitrile;dihydrochloride |
SDF | Download SDF |
Canonical SMILES | C1CC(N(C1)C(=O)CNCCNC2=NC=C(C=C2)C#N)C#N.Cl.Cl |
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 | NVP DPP 728 dihydrochloride是DPP-IV的强效的和口服有效的抑制剂,Ki和IC50值分别为11 nM和14 nM。 | |||||
靶点 | DPP-IV | |||||
IC50 | 14 nM (Ki = 11 nM) |
质量控制和MSDS
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