AVE 0991
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.
- 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Mas-transfected COS cells |
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Preparation method |
The solubility of this compound in DMSO is > 29mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
10-6 M |
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Applications |
AVE 0991 competed the specific binding of 125I-Ang-(1-7) to Mas-transfected COS cells with an IC50 value of 4.75 × 10-8 M. In addition, at the dose of 10-6 M, AVE 0991 completely abolished the specific binding of rhodamine-labeled Ang-(1-7) to Mas-transfected CHO cells. |
| Animal experiment [1]: | |
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Animal models |
Water-loaded WT mice (C57BL/6) |
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Dosage form |
0.58 nmol/g; i.p. |
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Applications |
In water-loaded WT mice (C57BL/6), AVE 0991 significantly decreased water dieresis, which was associated with an increase in urine osmolality. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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| 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 | |||||
Quality Control & MSDS
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