2049973-02-4
2049973-02-4 structure
- Name: AM-8123
- Chemical Name: AM-8123
- CAS Number: 2049973-02-4
- Molecular Formula: C27H33N7O5S
- Molecular Weight: 567.66
- Catalog: Research Areas Cardiovascular Disease
- Create Date: 2022-01-01 10:30:10
- Modify Date: 2024-01-16 20:18:23
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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].
| Name | AM-8123 |
|---|
| 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]. |
|---|---|
| Related Catalog | |
| 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]. |
| 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. |
| References |
| Molecular Formula | C27H33N7O5S |
|---|---|
| Molecular Weight | 567.66 |