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AP 811 is a high affinity, selective ANP clearance receptor (NPR3) antagonist (Ki = 0.45 nM). Exhibits >20,000-fold selectivity for NPR3 over NPR1. Inhibits ANP-stimulated Na+/K+ pump activity in rabbit ventricular cardiomyocytes in vitro. Also blocks proliferation of rodent neonatal cardiomyocytes seen at low ANP concentrations in vitro.
(Modifications: Arg-1 = N2-[4-(2-Naphthoylamino)phenylacetyl], Arg-4 = C-terminal (S)-2-methylbutylamide)
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solubility||Soluble to 1 mg/ml in water|
References are publications that support the biological activity of the product.
Veale et al (2000) The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. Part 1. Bioorg.Med.Chem.Lett. 10 1949 PMID: 10987424
William et al (2008) Natriuretic peptides stimulate the cardiac sodium pump via NPR-C-coupled NOS activation. Am.J.Physiol.Cell Physiol. 294 C1067 PMID: 18272821
Becker et al (2014) Differential activation of natriuretic peptide receptors modulates cardiomyocyte proliferation during development. Development 141 335 PMID: 24353062
If you know of a relevant reference for AP 811, please let us know.
Keywords: AP 811, AP 811 supplier, AP811, NPR3, ANP-CR, atrial, natriuretic, peptides, clearance, receptor, antagonists, antagonism, selective, high, affinity, Natriuretic, Peptide, Receptor, 5498, Tocris Bioscience
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Investigation of NPR3 agonism in blood vessels.
AP811 is extremely unstable. Shipped at RT as powder, but need to be frozen upon arrival and made fresh each time.
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