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AM-8123 

Cat. No.: HY-139486
Handling Instructions

AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease.

For research use only. We do not sell to patients.

AM-8123 Chemical Structure

AM-8123 Chemical Structure

CAS No. : 2049973-02-4

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Description

AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease[1].

IC50 & Target

APJ[1]

In Vitro

AM-8123 (100 nM) causes a rapid β-arrestin translocation from cytoplasm to plasma membrane in APJ-expressing cells. AM-8123 bound the native hAPJ receptor with low nanomolar affinity[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AM-8123 (100 mg/kg; p.o.) results in sustained improvement in systolic function and decreases both EDV and ESV as measured by echocardiography but not by the invasive pressure-volume conductance catheter at study termination[1].
AM-8123 (0.035, 0.09, 0.9, and 9 mg/kg; i.v.) improves cardiovascular function[1].
AM-8123 exhibits appreciably greater oral bioavailability in rats and dogs relative to pyr-apelin-13. AM-8123 infusion results in an increase in EF, SV, and dP/dt max at submicromolar unbound plasma concentrations with minimal change in HR, indicating that acute infusion of AM-8123 is associated with an improvement in several markers of cardiac function. AM-8123 is a more potent mediator of both ERK and AKT phosphorylation relative to pyr-apelin-13[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Lewis rats (2~3 months old)[1]
Dosage: 100 mg/kg
Administration: P.o.
Result: Resulted in sustained improvement in systolic function.
Decreased both EDV and ESV as measured by echocardiography but not by the invasive pressure-volume conductance catheter at study termination.
Animal Model: Rats[1]
Dosage: 0.035, 0.09, 0.9, and 9 mg/kg
Administration: I.v.
Result: Improved cardiovascular function.
Molecular Weight

567.66

Formula

C₂₇H₃₃N₇O₅S

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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AM-8123
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