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编 号：F748528
分子式：C27H33N7O5S
分子量：567.66
分子式：C27H33N7O5S
分子量：567.66
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CAS No: 2049973-02-4
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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 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.
体内研究：
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.
体外研究：
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.
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