AM-8123

Research use only, not for human use.

AM-8123 is an orally available nonpeptide APJ agonist.AM-8123 reduces collagen load and improves cardiac function.

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.

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.

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.AM-8123 (0.035, 0.09, 0.9, and 9 mg/kg; i.v.) improves cardiovascular function.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.Animal Model:Lewis rats (2~3 months old) 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 Dosage:0.035, 0.09, 0.9, and 9 mg/kg Administration:I.v.Result:Improved cardiovascular function.

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Others

Other Targets

Apelin receptor

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2049973-02-4

567.66

C27H33N7O5S

>98% (HPLC)

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N(S([C@H]([C@@H](OC(C)C)C=1N=CC(C)=CN1)C)(=O)=O)C=2N(C(=NN2)C=3C=C(C)C=NC3)C4=C(OC)C=CC=C4OC

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(-20℃)

With Ice Pack

≥ 2 years