Aplidine

CAS No. 137219-37-5

Aplidine( Plitidepsin )

Catalog No. M28854 CAS No. 137219-37-5

Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM). Aplidine is a potent anti-cancer agent by targeting eukaryotic translation elongation factor 1 Alpha 2(EEF1A2, Kd = 80?nM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Aplidine
  • Note
    Research use only, not for human use.
  • Brief Description
    Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM). Aplidine is a potent anti-cancer agent by targeting eukaryotic translation elongation factor 1 Alpha 2(EEF1A2, Kd = 80?nM).
  • Description
    Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM). Aplidine is a potent anti-cancer agent by targeting eukaryotic translation elongation factor 1 Alpha 2(EEF1A2, Kd = 80?nM).(In Vitro):In hACE2-293T cells, Aplidine exhibits anti–SARS-CoV-2 activity with an IC90 of 0.88 nM. In an established model of human pneumocyte-like cells, Aplidine inhibits SARS-CoV-2 replication with an IC90 of 3.14 nM and a selectivity index of 40.4. Aplidine (20 nM; 1 h) induces a dose-dependent decrease in VEGF secretion in MOLT-4 cells. Aplidine (20 nM; 1 h) does not result in significant inhibition of VEGF-R1 mRNA in normal endothelial cells, which do express VEGFR-1 but do not secrete VEGF.(In Vivo):In BALB/c mice expressing human ACE2, Aplidine significantly reduced SARS-CoV-2 infection. 0.3 mg/kg Aplidine group results in a reduction of nearly 2 log units in SARS-CoV-2 viral titers in the lungs, and the 1 mg/kg group leads to a reduction of 1.5 log units.
  • In Vitro
    ——
  • In Vivo
    Animal Model:BALB/c mice Dosage:0.3 mg/kg; 1 mg/kg Administration:1 day QD at 1 mg/kg; 3days QD at 0.3 mg/kg Result:Showed in vivo antiviral efficacy in mouse models of SARS-CoV-2 infection.
  • Synonyms
    Plitidepsin
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    EP1
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    137219-37-5
  • Formula Weight
    1110.34
  • Molecular Formula
    C57H87N7O15
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (90.06 mM)
  • SMILES
    CC[C@@H]([C@@H]1[C@@H](O)CC(O[C@@H](C(C)C)C([C@H](C)C(N[C@@H](CC(C)C)C(N2CCC[C@H]2C(N(C)[C@@H](CC3=CC=C(OC)C=C3)C(O[C@H](C)[C@H](NC([C@H](N(C([C@@H]4CCCN4C(C(C)=O)=O)=O)C)CC(C)C)=O)C(N1)=O)=O)=O)=O)=O)=O)=O)C
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.McKeown SC, et al. Identification of novel pyrazole acid antagonists for the EP1 receptor. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4767-7Epub 2006 Jul 14.
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