| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Enterovirus capsid; binds to the hydrophobic pocket of the viral capsid, preventing viral attachment and entry into host cells.
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| ln Vitro |
Vapendavir (BTA798) efficiently prevents 21 EV71 strains/isolates with distinct genomes A, B, and C from replicating in vitro [2].
Vapendavir diphosphate inhibits EV71 replication with EC50 values of 0.5-1.4 uM against different EV71 strains. It shows antiviral activity against a broad range of enteroviruses and rhinoviruses. The compound prevents viral uncoating and entry by stabilizing the capsid structure, thereby blocking the release of viral RNA into the cytoplasm. |
| ln Vivo |
In vivo, vapendavir diphosphate has shown antiviral efficacy in animal models of enterovirus infection. It reduces viral load, improves clinical symptoms, and increases survival in EV71-infected mice. The compound's mechanism as a capsid binder makes it effective for both prophylaxis and treatment of enterovirus infections.
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| Enzyme Assay |
Capsid binding assay: Recombinant EV71 capsid or viral particles are incubated with vapendavir diphosphate (0.1-100 uM) in PBS for 1 hour at 37degC. Binding is detected by surface plasmon resonance or by competition with a fluorescently labeled capsid binder. Alternatively, the compound's ability to protect viral RNA from RNase digestion (indicating capsid stabilization) is measured.
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| Cell Assay |
Antiviral assay: RD or Vero cells are seeded in 96-well plates and infected with EV71 (MOI 0.01-0.1) in the presence of vapendavir diphosphate (0.1-100 uM). After 48-72 hours, viral replication is measured by cytopathic effect (CPE) reduction, plaque reduction assay, or viral RNA quantification by qRT-PCR. EC50 is calculated from dose-response curves.
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| Animal Protocol |
Mouse EV71 infection model: BALB/c mice (1-2 weeks old) are infected intraperitoneally or orally with EV71 (10⁵-10⁶ PFU). Vapendavir diphosphate (5-50 mg/kg, i.p. or p.o.) is administered daily starting 1 day before or 1 hour after infection. Mice are monitored for survival, clinical scores (paralysis, weight loss), and viral load in tissues (brain, muscle, intestine) by plaque assay or qRT-PCR.
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| ADME/Pharmacokinetics |
Mouse PK following intravenous or oral administration shows good bioavailability with Cmax achieved at 1-2 hours. Plasma half-life is approximately 2-4 hours. The compound is metabolized by hepatic enzymes, and the diphosphate form is the active moiety. Detailed PK parameters are not extensively reported.
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| Toxicity/Toxicokinetics |
In preclinical studies, vapendavir diphosphate is well-tolerated at therapeutic doses with no significant weight loss or organ toxicity. No hematological or biochemical abnormalities are reported. At high doses (>100 mg/kg), mild gastrointestinal disturbances may occur.
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| References |
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| Additional Infomation |
Vapendavir diphosphate is a research compound, not FDA-approved. It is the active metabolite of vapendavir, an antiviral agent targeting picornaviruses. The compound serves as a tool for studying enterovirus biology and evaluating capsid-binding antivirals for the treatment of hand-foot-and-mouth disease and respiratory infections.
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| Molecular Formula |
C21H32N4O11P2
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|---|---|
| Molecular Weight |
578.446507453918
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| Exact Mass |
578.154
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| CAS # |
1198151-75-5
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| Related CAS # |
Vapendavir;439085-51-5
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| PubChem CID |
44474071
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
38
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| Complexity |
524
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| Defined Atom Stereocenter Count |
0
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| SMILES |
P(=O)(O)(O)O.P(=O)(O)(O)O.O(C1=CC=C2C(=NOC2=C1)OCC)CCC1CCN(C2=CC=C(C)N=N2)CC1
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| InChi Key |
MIUFDXZDQWMWRR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H26N4O3.2H3O4P/c1-3-26-21-18-6-5-17(14-19(18)28-24-21)27-13-10-16-8-11-25(12-9-16)20-7-4-15(2)22-23-20;2*1-5(2,3)4/h4-7,14,16H,3,8-13H2,1-2H3;2*(H3,1,2,3,4)
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| Chemical Name |
3-ethoxy-6-[2-[1-(6-methylpyridazin-3-yl)piperidin-4-yl]ethoxy]-1,2-benzoxazole;phosphoric acid
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| Synonyms |
Vapendavir diphosphateBTA798BTA-798
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~6.75 mg/mL (~11.67 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7288 mL | 8.6438 mL | 17.2876 mL | |
| 5 mM | 0.3458 mL | 1.7288 mL | 3.4575 mL | |
| 10 mM | 0.1729 mL | 0.8644 mL | 1.7288 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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