AVE 0991
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.
AVE 0991是血管紧张素-（1-7）受体的激动剂[1]。
作为血管紧张素-（1-7）的模拟物，AVE0991是血管紧张素-（1-7）受体的非肽类激动剂。在水负荷小鼠（C57BL / 6）中，AVE0991（0.58 nmol/g）显著减少水利尿。AVE的抗利尿效应与尿渗透压的增加相关。AVE0991在水负荷Swiss小鼠中也具有抗利尿效应。AVE的抗利尿效应可以被血管紧张素Ⅱ（Ang II）的拮抗剂完全阻断，表明AVE 0991的特异性。Ang II促进动脉粥样硬化，而血管紧张素-（1-7）与Ang II的作用相反。据报道，AVE 0991可以抑制载脂蛋白E（apoE）敲除小鼠模型中动脉粥样硬化[1，2]。
参考文献：
[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.
- 1. Sanket Patel, Tahir Hussain, et al. "Synergism between Angiotensin receptors ligands: Role of Angiotensin‐(1‐7) in modulating AT2R agonist response on nitric oxide in kidney cells." Pharmacol Res Perspect. 2020 Dec;8(6):e00667. PMID:33197136
- 2. Ming Zhang, Xintao Zhu, et al. "AVE 0991 Attenuates Pyroptosis and Liver Damage after Heatstroke by Inhibiting the ROS-NLRP3 Inflammatory Signalling Pathway." BioMed Research International. Volume 2019, Article ID 1806234, 12 pages.
- 3. Foulquier S, Caolo V, et al. "The role of receptor MAS in microglia-driven retinal vascular development." Angiogenesis. 2019 Jun 20. PMID:31240418
- 4. 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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 580.72 |
| Cas No. | 304462-19-9 |
| Formula | C29H32N4O5S2 |
| Solubility | ≥29.04 mg/mL in DMSO |
| Chemical Name | 1-ethyl-3-[3-[4-[(5-formyl-4-methoxy-2-phenylimidazol-1-yl)methyl]phenyl]-5-(2-methylpropyl)thiophen-2-yl]sulfonylurea |
| SDF | Download SDF |
| Canonical SMILES | CCNC(=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 | 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。 |
| 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. |
|
| 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 | |||||
质量控制和MSDS
- 批次:
化学结构
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