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Synonyms: Plitidepsin


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $247 | In Stock | In Stock | |
| 5 mg | $619 | In Stock | In Stock | |
| 10 mg | $828 | In Stock | In Stock | |
| 25 mg | $1,280 | In Stock | In Stock | |
| 50 mg | $1,650 | In Stock | In Stock | |
| 100 mg | $2,660 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $987 | In Stock | In Stock |
| 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). |
| Targets & IC50 | SARS-CoV-2:0.88 nM(IC90), eEF1A2:80 nM(Kd) |
| 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[1]. 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[1]. |
| 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[2]. |
| Synonyms | Plitidepsin |
| Molecular Weight | 1110.34 |
| Formula | C57H87N7O15 |
| Cas No. | 137219-37-5 |
| Smiles | [H][C@@]12CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@@H](C)C(=O)[C@@H](OC(=O)C[C@H](O)[C@]([H])(NC(=O)[C@@H](NC(=O)[C@@H](CC(C)C)N(C)C(=O)[C@@H]1CCCN1C(=O)C(C)=O)[C@@H](C)OC(=O)[C@H](Cc1ccc(OC)cc1)N(C)C2=O)[C@@H](C)CC)C(C)C |
| Relative Density. | 1.24 g/cm3 (Predicted) |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (45.03 mM), Sonication is recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 3.3 mg/mL (2.97 mM), Sonication is recommended. 10% DMSO+90% (20% SBE-β-CD in Saline): < 5 mg/mL (4.5 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+90% Saline: < 5 mg/mL (4.5 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: < 5 mg/mL (4.5 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+90% Corn oil: 5 mg/mL (4.5 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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