| Identification | Back Directory | [Name]
AVE 0991 (sodiuM salt) | [CAS]
306288-04-0 | [Synonyms]
AVE0991.Na salt
AVE 0991 Sodium
AVE 0991 (sodiuM salt)
ethylcarbamoyl-[3-[4-[(5-formyl-4-methoxy-2-phenylimidazol-1-yl)methyl]phenyl]-5-(2-methylpropyl)thiophen-2-yl]sulfonylazanide
N-[(Ethylamino)carbonyl]-3-[4-[(5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl]phenyl]-5-(2-methylpropyl)-2-thiophenesulfonamide monosodium salt | [Molecular Formula]
C29H31N4O5S2.Na | [MDL Number]
MFCD28167715 | [MOL File]
306288-04-0.mol | [Molecular Weight]
604.72 |
| Hazard Information | Back Directory | [Uses]
AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [125I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC50 of 21 nM[1]. | [Biological Activity]
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] | [target]
IC50: 21±35 nM (Ang-(1-7) receptor) | [IC 50]
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. | [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. |
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