AVE 0991 is an orally active, non-peptide-based selective Ang (1-7) receptor (Mas, MasR) agonist with 5-times NO-inducing efficacy than Ang (1-7) in bovine aortic endothelial cell (BAEC) cultures (10 μM; BAEC) and 10-fold higher affinity (IC50 = 21 nM vs 220 nM, respectively, against 10 nM [125I]-Ang-(1-7) for BAEC membrane binding), exhibiting little affinity toward AT1 & AT2 receptors. AVE 0991 is a widely probing Mas-mediated responses in cultures (0.01-10 μM) and in animal disease models in vivo (0.3-10 mg/kg via ip., po. or intranasal; rats and mice).
Orally active, non-peptide-based selective Ang (1-7) receptor (Mas, MasR) agonist in vitro and in vivo.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Recent work has renewed interest in therapies targeting the renin-angiotensin system (RAS) to improve β-cell function in type 2 diabetes. Studies show that generation of angiotensin-(1-7) by ACE2 and its binding to the Mas receptor (MasR) improves glucose homeostasis, partly
Recently, we demonstrated that the heptapeptide angiotensin-(1-7) (Ang-[1-7]) exhibits a favorable kinetic of nitric oxide (NO) release accompanied by extremely low superoxide (O2-) production. In this report we describe AVE 0991, a novel nonpeptide compound that evoked effects similar to
During the aging process, chronic neuroinflammation induced by microglia is detrimental for the brain and contributes to the etiology of several aging-related neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. As a newly identified axis of renin-angiotensin system, ACE2/Ang-(1-7)/MAS1
American journal of physiology. Heart and circulatory physiology, 312(5), H980-H991 (2017-04-16)
The objectives of the present study were to investigate the effect of ANG-(1-7) on the development of cardiac hypertrophy and to identify the intracellular mechanism underlying this action of ANG-(1-7). Blood pressure and heart rate were recorded using radiotelemetry before
Frontiers in pharmacology, 10, 146-146 (2019-03-12)
The MasR receptor (MasR) is an orphan G protein-coupled receptor proposed as a candidate for mediating the angiotensin (Ang)-converting enzyme 2-Ang-(1-7) protective axis of renin-angiotensin system. This receptor has been suggested to participate in several physiological processes including cardio- and
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