Aplidine

SKU: orb1297925

Description

Aplidine

Research Area

Product Categories/Products/Small Molecules,Cell Cycle/Checkpoint|||Microbiology/Virology|||DNA Damage/DNA Repair

Key Properties

• CAS Number: 137219-37-5
• MW: 1110.34
• Purity: 98.12%
• Formula: C₅₇H₈₇N₇O₁₅
• 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

Bioactivity

• Target IC50:
  SARS-CoV-2:0.88 nM(IC90)|eEF1A2:80 nM(Kd)
• 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 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.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Compound Identifiers

PubChem CID

9812534