A 779

A 779

Catalog Number:
L002371404APE
Mfr. No.:
APE-B6056
Price:
$185
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          Background

          A 779 is a potent and selective angiotensin-(1-7)/ Mas receptor antagonist [1].Angiotensin-(1-7) is a bioactive component of the renin angiotensin system (RAS) which plays an important role in cardiovascular homeostasis and hydroelectrolyte balance in physiological and pathologic conditions [1][2].A 779 is an angiotensin antagonist selective for the heptapeptide angiotensin-(I-7) [Ang-(l-7)] [1]. In water-loaded rats, A 779 significantly inhibited the antidiuretic effect of Ang-(l-7). In the rostral ventrolateral medulla, A-779 completely blocked the pressor effect produced by Ang-(1-7) microinjection [1]. In conscious Wistar rats, infusion of vehicle or A-779 (80 ng/ min, i.v.) started 40 to 45 minutes after captopril administration produced a significant shift of the BK dose-response curve obtained after captopril. A-779 significantly attenuated the potentiation of the hypotensive effect of BK by the ACE inhibitor captopril in conscious rats [2]. In anaesthetized male Wistar rats, when AT1R and AT2R were blocked, A779 increased renal blood flow/wet kidney tissue weight (RBF/KW). Co-blockade of all AT1R, AT2R, and MasR might alter RBF/ KW in male more than in female rats, which supported a crosstalk between MasR and Ang II receptors in renal circulation [3].

          Santos RA, Campagnole-Santos MJ, Baracho NC, et al. Characterization of a new angiotensin antagonist selective for angiotensin-(1-7): evidence that the actions of angiotensin-(1-7) are mediated by specific angiotensin receptors. Brain Res Bull. 1994;35(4):293-8.
          Maia LG, Ramos MC, Fernandes L, et al. Angiotensin-(1-7) antagonist A-779 attenuates the potentiation of bradykinin by captopril in rats. J Cardiovasc Pharmacol. 2004 May;43(5):685-91.
          Mansoori A, Oryan S, Nematbakhsh M. Role of Mas receptor antagonist (A779) in renal hemodynamics in condition of blocked angiotensin II receptors in rats. Acta Physiol Hung. 2016 Mar;103(1):13-20.

      • Properties
        • Categories
          angiotensin-(1-7)/ Mas receptor antagonist
          Alternative Name
          (2R,3Z,5S,6Z,8S,9Z,11S,12Z,14S,15Z,17S,18Z,20S)-5-((1H-imidazol-5-yl)methyl)-20-amino-8-((S)-sec-butyl)-17-(3-guanidinopropyl)-4,7,10,13,16,19-hexahydroxy-11-(4-hydroxybenzyl)-14-isopropyl-2-methyl-3,6,9,12,15,18-hexaazadocosa-3,6,9,12,15,18-hexaene-1,22-
          CAS Number
          159432-28-7
          Molecular Formula
          C39H60N12O11
          Molecular Weight
          872.97
          Purity
          98.17%
          Solubility
          ≥29.1 mg/mL in H2O with gentle warming; insoluble in EtOH; ≥44.7 mg/mL in DMSO
          Storage
          Store at -20°C
          SMILES
          CC[[email protected]]([[email protected]@](/N=C(O)/[[email protected]](/N=C(O)/[[email protected]](/N=C(O)/[[email protected]](/N=C(O)/[[email protected]](N)([H])CC(O)=O)([H])CCCNC(N)=N)([H])C(C)C)([H])CC1=CC=C(O)C=C1)([H])/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]](C(O)=O)([H])C)([H])CC2=CN=CN2)([H])C

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