| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Pleconaril (also known as VP 63843; Win 63843) is a capsid inhibitor and an antiviral drug that has the potential for the treatment of enterovirus infection and asthma. Pleconaril is effective in inhibiting replication with an IC50 of 50 nM. Pleconaril, administered either orally or intranasally, is active against viruses in the Picornaviridae family, including Enterovirus and Rhinovirus.It has shown useful activity against the dangerous strain enterovirus D68. Pleconaril has been used as treatment on a compassionateuse basis in neonates and immunodeficient patients with severe EV infections.
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| ln Vivo |
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| Animal Protocol |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
70% (oral) |
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| Toxicity/Toxicokinetics |
Protein Binding
>99% |
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| References |
Virol J.2015 Jul 14;12:106.J Gen Virol.2015 Mar;96(Pt 3):571-9.
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| Additional Infomation |
Pleconaril is an antiviral drug from viral capsid inhibitor class, manufactured by Schering-Plough and intended for the prevention of acute asthma exacerbations and common cold symptoms in asthmatic patients who have had exposure to picornavirus. It acts by inhibiting viral replication. The use of pleconaril has not gained approval by the U.S. Food and Drug Administration (FDA) due to the fact that it has been found to induce CYP3A enzyme activity, therefore increasing the risk for serious drug interactions.
Pleconaril has been reported in Isatis tinctoria with data available. Pleconaril is a small-molecule inhibitor with activity against viruses in the picornaviridae family, including enterovirus and rhinovirus. Pleconaril binds to a hydrophobic pocket in the major capsid protein and prevents uncoating of the viral RNA genome. In enteroviruses it also prevents the virus from attaching itself to the host cell. Drug Indication Investigated for use/treatment in upper respiratory infection. Mechanism of Action Pleconaril binds to a hydrophobic pocket in viral protein 1, the major protein which makes up the capsid (shell) of picornaviruses. This renders the viral capsid rigid and compressed and prevents the uncoating of its RNA. As a result, the virus is stopped from attaching to the host cell and causing infection. |
| Molecular Formula |
C18H18F3N3O3
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| Molecular Weight |
381.35
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| Exact Mass |
381.13
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| Elemental Analysis |
C, 56.69; H, 4.76; F, 14.95; N, 11.02; O, 12.59
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| CAS # |
153168-05-9
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| Related CAS # |
Pleconaril-d4;2749329-20-0
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| PubChem CID |
1684
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| Appearance |
White to biege solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
481.2±55.0 °C at 760 mmHg
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| Melting Point |
61-62°
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| Flash Point |
244.8±31.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.509
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| LogP |
5.77
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
471
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1=NC(C2C([H])=C(C([H])([H])[H])C(=C(C([H])([H])[H])C=2[H])OC([H])([H])C([H])([H])C([H])([H])C2=C([H])C(C([H])([H])[H])=NO2)=NO1)(F)F
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| InChi Key |
KQOXLKOJHVFTRN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H18F3N3O3/c1-10-7-13(16-22-17(27-24-16)18(19,20)21)8-11(2)15(10)25-6-4-5-14-9-12(3)23-26-14/h7-9H,4-6H2,1-3H3
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| Chemical Name |
3-(3,5-dimethyl-4-(3-(3-methylisoxazol-5-yl)propoxy)phenyl)-5-(trifluoromethyl)-1,2,4-oxadiazole
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 76~100 mg/mL ( 199.29~262.23 mM )
Ethanol : 76 mg/mL Water : ˂1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10% DMSO+90% Corn Oil: ≥ 2.5 mg/mL (6.56 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6223 mL | 13.1113 mL | 26.2226 mL | |
| 5 mM | 0.5245 mL | 2.6223 mL | 5.2445 mL | |
| 10 mM | 0.2622 mL | 1.3111 mL | 2.6223 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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