AP 811 acetate
AP 811 acetate is a selective atrial natriuretic peptide clearance receptor (ANP-CR, NPR3) antagonist with a Ki of 0.48 nM. AP 811 acetate displays >20000-fold selectivity for NPR3 over NPR1. AP 811 acetate abolishes ANP-induced pump stimulation.
For research use only. We do not sell to patients.
- Formula: C46H66N12O8.xC2H4O2
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
Ki: 0.48 nM (NPR3)[1]
In Vitro
In proliferating cardiomyocytes, AP 811 acetate (10-500 nM) could completely abolish the enhanced cardiomyocyte proliferation seen with low concentration ANP (10 nM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
-
Formula C46H66N12O8.xC2H4O2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
Purity & Documentation
References
[1]. Veale CA, et al. The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. Part 1. Bioorg Med Chem Lett. 2000;10(17):1949-1952. [Content Brief]
[2]. William M, et al. Natriuretic peptides stimulate the cardiac sodium pump via NPR-C-coupled NOS activation. Am J Physiol Cell Physiol. 2008;294(4):C1067-C1073. [Content Brief]
[3]. Jason R Becker, et al. Differential activation of natriuretic peptide receptors modulates cardiomyocyte proliferation during development. Development. 2014 Jan;141(2):335-45. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)