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AM-8123
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AM-8123图片
CAS NO:2049973-02-4
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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。
生物活性

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

IC50& Target

APJ[1]

体外研究
(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].

体内研究
(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].

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.
分子量

567.66

Formula

C27H33N7O5S

CAS 号

2049973-02-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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