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AVE 0991

现货
Catalog No.
B1007
血管紧张素-(1-7)受体激动剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 3,150.00
Ship with 10-15 days
5mg
¥ 2,380.00
Ship with 10-15 days
10mg
¥ 3,610.00
Ship with 10-15 days
25mg
¥ 5,230.00
Ship with 10-15 days
50mg
¥ 8,550.00
Ship with 10-15 days
100mg
¥ 13,300.00
Ship with 10-15 days

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Background

AVE 0991 is an agonist of angiotensin-(1-7) receptor [1].

As an ang-(1–7) mimic, AVE0991 acts as a nonpeptide agonist of angiotensin-(1-7) receptor. In water-loaded mice (C57BL/6), AVE0991(0.58 nmol/g)produces a significant decrease of water dieresis. The antidiuretic effect of AVE was associated with an increase in urine osmolality. It also occurs in water-loaded Swiss mice. The antidiuretic action of AVE can be blocked by the Ang II antagonists completely, demonstrating the specificity of AVE 0991. Since Ang II promotes atherogenesis and ang-(1–7) opposites Ang II action, it is reported that AVE 0991 can inhibit atherogenesis in apolipoprotein E (apoE)-knockout mice model [1, 2].

References:
[1] Sergio Veloso Brant Pinheiro, Ana Cristina Simoes e Silva, Walkyria Oliveira Sampaio, Renata Dutra de Paula, Elizabeth Pereira Mendes, Elizabete Dias Bontempo, Joao Bosco Pesquero, Thomas Walther, Natalia Alenina, Michael Bader, Markus Bleich, Robson Augusto Souza Santos. Nonpeptide AVE 0991 Is an Angiotensin-(1–7) Receptor Mas Agonist in the Mouse Kidney. Hypertension. 2004, 44: 490-496.
[2] J. Toton-Zuranska, M. Gajda, G. Pyka-Fosciak, K. Kus, M. Pawlowska, A. Niepsuj, P. Wolkow, R. Olszanecki, J. Jawien, R. Korbut. AVE 0991- angiotensin-(1-7) receptor agonist, inhibits atherogenesis in APOE-knockout mice. Journal of physiology and pharmacology. 2010, 61(2):181-183.

文献引用

1. Burghi V, Echeverría EB, et al. "Participation of Gα(i)-Adenylate Cyclase and ERK1/2 in Mas Receptor Signaling Pathways." Front Pharmacol. 2019 Feb 22;10:146. PMID:30853914

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt580.72
Cas No.304462-19-9
FormulaC29H32N4O5S2
Solubility≥29.036mg/mL in DMSO
Chemical Name1-ethyl-3-[3-[4-[(5-formyl-4-methoxy-2-phenylimidazol-1-yl)methyl]phenyl]-5-(2-methylpropyl)thiophen-2-yl]sulfonylurea
SDFDownload SDF
Canonical SMILESCCNC(=O)NS(=O)(=O)C1=C(C=C(S1)CC(C)C)C2=CC=C(C=C2)CN3C(=C(N=C3C4=CC=CC=C4)OC)C=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

细胞实验 [1]:

细胞系

转染Mas的COS细胞

制备方法

在DMSO中的溶解度大于29 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

10-6 M

实验结果

AVE 0991与125I-Ang-(1-7)竞争结合转染Mas的COS细胞的特异性结合位点,其IC50值为4.75 × 10-8 M。此外,在10-6 M的剂量下,AVE 0991完全抑制罗丹明标记的Ang-(1-7)与转染Mas的COS细胞之间的特异性结合。

Animal experiment [1]:

Animal models

喝饱水的WT小鼠 (C57BL/6)

Dosage form

0.58 nmol/g;腹腔注射

Applications

在喝饱水的WT小鼠 (C57BL/6) 中,AVE 0991显著减少水渗透,上述作用与尿渗透压增加相关。

Other notes

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Sergio Veloso Brant Pinheiro, Ana Cristina Simoes e Silva, Walkyria Oliveira Sampaio, Renata Dutra de Paula, Elizabeth Pereira Mendes, Elizabete Dias Bontempo, Joao Bosco Pesquero, Thomas Walther, Natalia Alenina, Michael Bader, Markus Bleich, Robson Augusto Souza Santos. Nonpeptide AVE 0991 Is an Angiotensin-(1–7) Receptor Mas Agonist in the Mouse Kidney. Hypertension. 2004, 44: 490-496.

生物活性

描述 AVE 0991是血管紧张素-(1-7)受体的激动剂,IC50值为21 nM。
靶点 angiotensin-(1-7) receptor          
IC50 21 nM          

质量控制

化学结构

AVE 0991

相关生物数据

AVE 0991