AM-8123

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AM-8123 是一种口服有效的 APJ 激动剂。AM-8123 抑制 Forskolin 诱导的 cAMP 的生成，促进 Gα 蛋白活化。AM-8123 可用于心血管疾病的研究。

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.

——

Others

Other Targets

Apelin receptor

——

——

2049973-02-4

567.66

C27H33N7O5S

>98% (HPLC)

——

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

——

(-20℃)

With Ice Pack

≥ 2 years