AVE 0991 sodium salt
IC50: AVE 0991 and Ang-(1–7) competitively bind to bovine aortic endothelial cell membranes with IC50 values of 21 ± 35 and 220 ± 280 nM, respectively.
Angiotensin-(1–7) (Ang-[1–7]) acts as a crucial component of the renin-angiotensin system which can regulate and maintain the blood pressure by offsetting effects of Ang II, a typical vasoconstrictor in vivo. AVE 0991, a nonpeptide mimic of Ang-(1–7), performs as an agonist of angiotensin-(1-7) receptor. It plays an important role in exploring effects of Ang-(1-7) and evaluating the potential of Ang-(1-7) as a cardiovascular drug. [1]
In vitro: AVE 0991 was found to compete with Ang-(1-7) for bovine aortic endothelial cell membrane receptors with an IC50 of 21±35 nM. There was no significant difference in peak concentrations of NO and O2- released from AVE 0991 treated group and Ang-(1-7) treated group. However, the released amount of NO was approximately 5 times higher in AVE 0991 group than that in Ang-(1-7) group. Moreover, AVE 0091 significantly displaced the binding of I-Ang-(1-7) in both Mas-transfected monkey kidney cells (COS) and Mas-transfected Chinese hamster ovary (CHO) cells. [1]
In vivo: AVE 0091 at a dosage of 0.58 nmol/g resulted in a significant decrease in urinary volume, together with an increase in urinary osmolality in water-loaded C57BL/6 mice. [2] The antidiuretic effect of AVE was completely offset by the Ang II antagonists, which indicting a high specificity of AVE 0991. Since Ang II induced atherogenesis and ang-(1–7) offset Ang II action, it was proved that AVE 0991 blocked atherogenesis in apolipoprotein E (apoE)-knockout mice model. [3]
Clinical trial: So far, no clinical trial has been conducted.
References:
[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+] |
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. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
