AVE 0991 sodium salt
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.
IC50值:AVE 0991和Ang-(1–7)与牛主动脉内皮细胞膜竞争性结合,IC50值分别为21 ± 35和220 ± 280 nM。
血管紧张素-(1–7) (Ang-[1–7])是肾素-血管紧张素系统的重要组成部分,而肾素-血管紧张素系统通过抵消血管紧张素Ⅱ(典型的体内血管收缩剂)的效应来调节和维持血压。作为血管紧张素-(1–7)的非肽类模拟物,AVE 0991是血管紧张素-(1-7)受体的激动剂。它在研究血管紧张素-(1-7)的作用和评估血管紧张素-(1-7)作为心血管药物的潜力方面具有重要作用[1]。
体外实验:研究发现,AVE 0991可与血管紧张素-(1-7)竞争牛主动脉内皮细胞膜受体,IC50值为21±35 nM。从AVE 0991处理组与血管紧张素-(1-7)处理组释放的NO和O2-峰值浓度没有显著差异。然而,AVE 0991处理组内NO的释放量比血管紧张素-(1-7)处理组内NO的释放量高约5倍。此外,AVE 0091显著置换Mas转染猴肾细胞(COS)和Mas转染中国仓鼠卵巢(CHO)细胞内血管紧张素I-(1-7)的结合[1]。
体内实验:在水负荷C57BL/6小鼠中,0.58 nmol/g 剂量的AVE 0091可显著减少尿量,且增加尿渗透压[2]。Ang II拮抗剂可完全抵消AVE的抗利尿作用,这表明,AVE 0991具有高特异性。由于Ang II可诱发动脉粥样硬化,而血管紧张素-(1-7)抵消Ang II的作用,经证实,在载脂蛋白E(ApoE)基因敲除小鼠模型中,AVE 0991阻止动脉粥样硬化[3]。
临床试验:到目前为止,还未进行临床试验。
参考文献:
[1]Wiemer G, Dobrucki LW, Louka FR, Malinski T, Heitsch H. AVE 0991, a nonpeptide mimic of the effects of angiotensin-(1–7) on the endothelium. Hypertension. 2002 Dec; 40: 847-52.
[2] Pinheiro SV, Silva AC, Sampaio WO, Paula RD, Mendes EP, Bontempo ED, Pesquero JB, Walther T, Alenina N, Bader M, Bleich M and Santos RA. Nonpeptide AVE 0991 is an angiotensin-(1-7) receptor Mas agonist in the mouse kidney. Hypertension. 2004 Oct; 44(4):490-6.
[3]Toton-Zuranska J, Gajda M, Pyka-Fosciak G, Kus K, Pawlowska M, Niepsuj A, Wolkow P, Olszanecki R, Jawien J and Korbut R. AVE 0991- angiotensin-(1-7) receptor agonist, inhibits atherogenesis in APOE-knockout mice. J Physiol Pharm. 2010, 61(2):181-183.
Storage | Store at -20°C |
M.Wt | 602.7 |
Cas No. | 306288-04-0 |
Formula | C29H31N4NaO5S2 |
Solubility | Soluble in DMSO |
Chemical Name | sodium (Z)-N'-ethyl-N-((3-(4-((5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl)phenyl)-5-isobutylthiophen-2-yl)sulfonyl)carbamimidate |
SDF | Download SDF |
Canonical SMILES | CC/N=C([O-])/NS(C1=C(C2=CC=C(CN3C(C=O)=C(OC)N=C3C4=CC=CC=C4)C=C2)C=C(S1)CC(C)C)(=O)=O.[Na+] |
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。 |