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Submit ReviewAP 811
Description: High affinity, selective NPR3 antagonist
Purity: ≥95% (HPLC)
Biological Activity for AP 811
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.
Technical Data for AP 811
| M. Wt | 915.1 |
| Formula | C46H66N12O8 |
| Sequence |
RIDR (Modifications: Arg-1 = N2-[4-(2-Naphthoylamino)phenylacetyl], Arg-4 = C-terminal (S)-2-methylbutylamide) |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 124833-45-0 |
| PubChem ID | 44301714 |
| InChI Key | UNMJSSQZDQBGDS-OCFLPWLCSA-N |
| Smiles | CC[C@H](C)CNC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)CC1=CC=C(NC(=O)C2=CC3=C(C=CC=C3)C=C2)C=C1)[C@@H](C)CC |
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 Data for AP 811
| Solubility | Soluble to 1 mg/ml in water |
Product Datasheets for AP 811
References for AP 811
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.
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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
2 Citations for AP 811
Citations are publications that use Tocris products. Selected citations for AP 811 include:
Wei et al (2021) Atrial Natriuretic Peptide Promotes Neurite Outgrowth and Survival of Cochlear Spiral Ganglion Neurons in vitro Through NPR-A/cGMP/PKG Signaling. Front Cell Dev Biol 9 681421 PMID: 34268307
Zhen et al (2021) C-Type Natriuretic Peptide Ameliorates Vascular Injury and Improves Neurological Outcomes in Neonatal Hypoxic-Ischemic Brain Injury in Mice. Int J Mol Sci 22 PMID: 34445671
Do you know of a great paper that uses AP 811 from Tocris? Please let us know.
Reviews for AP 811
Average Rating: 4 (Based on 1 Review.)
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Good NPR3 agonist.
By
Anonymous on 07/12/2018
Assay Type: Ex Vivo
Species: Rat
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.