AVE0991

Product NameAVE0991
CAS304462-19-9
MFC29H32N4O5S2
MW580.72
EINECS
MOL File304462-19-9.mol

Chemical Properties

Melting point	191-192℃
Density	1.31±0.1 g/cm3(Predicted)
storage temp.	under inert gas (nitrogen or Argon) at 2–8 °C
solubility	≥29.04 mg/mL in DMSO
form	solid
pka	5.12±0.10(Predicted)
color	Off-white to yellow

Usage And Synthesis

Biological Activity

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].

in vitro

AVE 0991 is a nonpeptide compound that evokes effects similar to Ang-(1-7) on the endothelium. AVE 0991 and unlabeled Ang-(1-7) compete for high-affinity binding of [ ¹²⁵ I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC ₅₀ s of 21±35 and 220±280 nM, respectively . Peak concentrations of NO and O ₂ ^- release by AVE 0991 sodium salt and Ang-(1-7) (both 10 μM) are not significantly different (NO: 295 ±20 and 270±25 nM; O ₂ ^- : 18±2 and 20±4 nM). However, the released amount of bioactive NO is ≈5 times higher for AVE 0991 in comparison to Ang-(1-7).

target

angiotensin-(1-7) receptor

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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