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AM-8123

Catalog No. T39442 CAS 2049973-02-4

AM-8123 is an APJ agonist with high oral bioavailability and potency. It effectively inhibits Forskolin-stimulated cAMP production and activates Gα proteins. This compound is valuable for cardiovascular disease research.

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AM-8123, CAS 2049973-02-4

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	AM-8123 is an APJ agonist with high oral bioavailability and potency. It effectively inhibits Forskolin-stimulated cAMP production and activates Gα proteins. This compound is valuable for cardiovascular disease research.
In vitro	AM-8123 (100 nM) swiftly induces β-arrestin relocation from the cytoplasm to the plasma membrane in cells expressing APJ. It also exhibits low nanomolar affinity binding to the native hAPJ receptor[1].
In vivo	AM-8123 administered orally at a dosage of 100 mg/kg in 2 to 3-month-old Lewis rats leads to a notable enhancement in systolic function, along with reduced end-diastolic volume (EDV) and end-systolic volume (ESV), as determined via echocardiography; however, these findings were not mirrored when using invasive pressure-volume conductance catheter measurements upon the study's completion[1]. Additionally, intravenous doses of AM-8123 (0.035, 0.09, 0.9, and 9 mg/kg) in rats were found to bolster cardiovascular function[1]. Notably, AM-8123 demonstrates significantly higher oral bioavailability in rats and dogs compared to pyr-apelin-13, and its infusion leads to increased ejection fraction (EF), stroke volume (SV), and maximal rate of pressure development (dP/dt max). These benefits occurred at submicromolar unbound plasma concentrations, with minimal fluctuations in heart rate (HR), signifying that AM-8123 acutely enhances several cardiovascular function indicators. Moreover, it has been identified as a more potent enhancer of ERK and AKT phosphorylation when compared to pyr-apelin-13[1].

Molecular Weight	567.67
Formula	C27H33N7O5S
CAS No.	2049973-02-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Ason B, et al. Cardiovascular response to small-molecule APJ activation. JCI Insight. 2020;5(8):e132898. Published 2020 Apr 23. doi:10.1172/jci.insight.132898

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AM-8123 2049973-02-4 AM8123 AM 8123 inhibitor inhibit

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