AVE 0991Agonist of angiotensin-(1-7) receptor CAS# 304462-19-9 |
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Quality Control & MSDS
3D structure
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| Cas No. | 304462-19-9 | SDF | Download SDF |
| PubChem ID | 9851724 | Appearance | Powder |
| Formula | C29H32N4O5S2 | M.Wt | 580.72 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 41.67 mg/mL (71.76 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | 1-ethyl-3-[3-[4-[(5-formyl-4-methoxy-2-phenylimidazol-1-yl)methyl]phenyl]-5-(2-methylpropyl)thiophen-2-yl]sulfonylurea | ||
| 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 | ||
| Standard InChIKey | QTOZBSNPDCWHPV-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C29H32N4O5S2/c1-5-30-29(35)32-40(36,37)28-24(16-23(39-28)15-19(2)3)21-13-11-20(12-14-21)17-33-25(18-34)27(38-4)31-26(33)22-9-7-6-8-10-22/h6-14,16,18-19H,5,15,17H2,1-4H3,(H2,30,32,35) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | AVE 0991 is an agonist of angiotensin-(1-7) receptor with IC50 value of 21 nM. | |||||
| Targets | angiotensin-(1-7) receptor | |||||
| IC50 | 21 nM | |||||
AVE 0991 Dilution Calculator
AVE 0991 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.722 mL | 8.61 mL | 17.22 mL | 34.44 mL | 43.05 mL |
| 5 mM | 0.3444 mL | 1.722 mL | 3.444 mL | 6.888 mL | 8.61 mL |
| 10 mM | 0.1722 mL | 0.861 mL | 1.722 mL | 3.444 mL | 4.305 mL |
| 50 mM | 0.0344 mL | 0.1722 mL | 0.3444 mL | 0.6888 mL | 0.861 mL |
| 100 mM | 0.0172 mL | 0.0861 mL | 0.1722 mL | 0.3444 mL | 0.4305 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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AVE 0991 attenuates cardiac hypertrophy through reducing oxidative stress.[Pubmed:26403967]
Biochem Biophys Res Commun. 2016 Jun 10;474(4):621-625.
AVE 0991, the nonpeptide angiotensin-(1-7) (Ang-(1-7)) analog, is recognized as having beneficial cardiovascular effects. However, the mechanisms have not been fully elucidated. This study was designed to investigate the effects of AVE 0991 on cardiac hypertrophy and the mechanisms involved. Mice were underwent aortic banding to induce cardiac hypertrophy followed by the administration of AVE 0991 (20 mg kg.day (-1)) for 4 weeks. It was shown that AVE 0991 reduced left ventricular hypertrophy and improved heart function, characterized by decreases in left ventricular weight and left ventricular end-diastolic diameter, and increases in ejection fraction. Moreover, AVE 0991 significantly down-regulated mean myocyte diameter and attenuate the gene expression of the hypertrophic markers. Furthermore, AVE 0991 inhibited the expression of NOX 2 and NOX 4, meaning that AVE 0991 reduced oxidative stress of cardiac hypertrophy mice. Our data showed that AVE 0991 treatment could attenuate cardiac hypertrophy and improve heart function, which may be due to reduce oxidative stress.
The influence of angiotensin-(1-7) peptidomimetic (AVE 0991) and nebivolol on angiotensin I metabolism in aorta of apoE-knockout mice.[Pubmed:23959728]
J Physiol Pharmacol. 2013 Jun;64(3):317-20.
The detrimental role of over activation of renin-angiotensin system (RAS) in atherogenesis is widely recognized. Recently, we have demonstrated that Ang-(1-7) peptidomimetic - AVE0991, as well as known beta-adrenolytic agent nebivolol, exert anti-atherogenic actions in mouse model of atherosclerosis - apoE-knockout mice. Here, using LC-ESI-MS ex vivo system, we tested whether prolonged treatment of apoE-knockout mice by these drugs can influence RAS in aorta of apoE-knockout mice in regard to generation of most active metabolites of Ang I-Ang II and Ang-(1-7). As compared to wild type animals there was increased generation of Ang II in aorta of apoE-knockout mice, while the formation of Ang-(1-7) did not differ between both groups. Either treatment with AVE0991 or nebivolol resulted in significant attenuation of Ang II production in aorta of apoE-knockout mice. In conclusion, for the first time we directly demonstrated that there is increase in ability of aortic tissue to generate Ang II in mouse model of atherosclerosis of apoE knockout mice, and that such effect could be efficiently attenuated either by treatment of nebivolol or Ang-(1-7) peptidomimetic - AVE0991. The exact mechanism(s) responsible for interference of both drugs with RAS require further investigation.
The influence of angiotensin-(1-7) Mas receptor agonist (AVE 0991) on mitochondrial proteome in kidneys of apoE knockout mice.[Pubmed:23988828]
Biochim Biophys Acta. 2013 Dec;1834(12):2463-9.
Excessive action of angiotensin II on mitochondria has been shown to play an important role in mitochondrial dysfunction, a common feature of atherogenesis and kidney injury. Angiotensin-(1-7)/Mas receptor axis constitutes a countermeasure to the detrimental effects of angiotensin II on AT1 receptors. The aim of the study was to assess the effects of angiotensin-(1-7) peptidomimetic AVE0991 on the kidney mitochondrial proteome in widely used animal model of atherosclerosis (apoE(-/-) mice). Proteins changed in apoE(-/-) mice belonged to the groups of antioxidant enzymes, apoptosis regulators, inflammatory factors and metabolic enzymes. Importantly, AVE0991 partially reversed atherosclerosis-related changes in apoE(-/-) mice.
AVE 0991, a non-peptide mimic of angiotensin-(1-7) effects, attenuates pulmonary remodelling in a model of chronic asthma.[Pubmed:23889691]
Br J Pharmacol. 2013 Oct;170(4):835-46.
BACKGROUND AND PURPOSE: AVE 0991 (AVE) is a non-peptide compound, mimic of the angiotensin (Ang)-(1-7) actions in many tissues and pathophysiological states. Here, we have investigated the effect of AVE on pulmonary remodelling in a murine model of ovalbumin (OVA)-induced chronic allergic lung inflammation. EXPERIMENTAL APPROACH: We used BALB/c mice (6-8 weeks old) and induced chronic allergic lung inflammation by OVA sensitization (20 mug.mouse(-1) , i.p., four times, 14 days apart) and OVA challenge (1%, nebulised during 30 min, three times per.week, for 4 weeks). Control and AVE groups were given saline i.p and challenged with saline. AVE treatment (1 mg.kg(-1) .per day, s.c.) or saline (100 muL.kg(-1) .per day, s.c.) was given during the challenge period. Mice were anaesthetized 72 h after the last challenge and blood and lungs collected. In some animals, primary bronchi were isolated to test contractile responses. Cytokines were evaluated in bronchoalveolar lavage (BAL) and lung homogenates. KEY RESULTS: Treatment with AVE of OVA sensitised and challenged mice attenuated the altered contractile response to carbachol in bronchial rings and reversed the increased airway wall and pulmonary vasculature thickness and right ventricular hypertrophy. Furthermore, AVE reduced IL-5 and increased IL-10 levels in the BAL, accompanied by decreased Ang II levels in lungs. CONCLUSIONS AND IMPLICATIONS: AVE treatment prevented pulmonary remodelling, inflammation and right ventricular hypertrophy in OVA mice, suggesting that Ang-(1-7) receptor agonists are a new possibility for the treatment of pulmonary remodelling induced by chronic asthma.
