AM-8123

CAS No. 2049973-02-4

AM-8123( —— )

Catalog No. M35118 CAS No. 2049973-02-4

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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2MG 445 Get Quote
5MG 686 Get Quote
10MG 938 Get Quote
25MG 1398 Get Quote
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Biological Information

  • Product Name
    AM-8123
  • Note
    Research use only, not for human use.
  • Brief Description
    AM-8123 is an orally available nonpeptide APJ agonist.AM-8123 reduces collagen load and improves cardiac function.
  • 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.
  • 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.
  • 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.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.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Apelin receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2049973-02-4
  • Formula Weight
    567.66
  • Molecular Formula
    C27H33N7O5S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    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
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Ason B, et al. Cardiovascular response to small-molecule APJ activation. JCI Insight. 2020;5(8):e132898. Published 2020 Apr 23. doi:10.1172/jci.insight.132898
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