| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Buparvaquone targets the mitochondrial electron transport chain in protozoan parasites. As a hydroxynaphthoquinone, it inhibits the cytochrome bc1 complex (complex III), disrupting the electron transport chain and ATP production. This leads to the death of the parasite. Its mechanism is similar to that of atovaquone.
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| ln Vitro |
In a 4-day proliferation study, buprovalone successfully reduced the reproduction of Neospora caninum tachyzoites (IC50=4.9 nM; IC100=100 nM) [1]. Buparvaquone has a notable degree of L selectivity. Intracellular amastigotes of (L.) infantum with an IC50 of 1.5 μM. Bupavalquinone also exhibits sensitivity in other skin species, with IC50 values ranging from 1-4 μM [2].
In vitro, Buparvaquone demonstrates potent antiprotozoal activity. It is effective against Theileria species, which cause theileriosis in livestock. Its activity is measured by its ability to inhibit the growth of the parasite in cell culture. Its IC50 values are characteristic of a potent antiprotozoal agent. It is more potent than its parent compound, Parvaquone. |
| ln Vivo |
mice with a N infection. Bupavalone (100 mg/kg) was administered intraperitoneally via injection or gavage to caninum patients. The intraperitoneal therapy group shielded four out of the six mice from neosporiasis signs. Six of the seven mice in the group did not develop neosporiasis symptoms after receiving oral medication. 1]. When compared to untreated controls, bupavalone hydrogels and water-in-oil emulsions dramatically decreased cutaneous parasite burden and lesion size [3].
In vivo, Buparvaquone is used in veterinary medicine for the treatment of theileriosis, a tick-borne disease in cattle and other livestock. It is administered by injection and is effective in clearing the parasite from the blood and tissues. Its efficacy has been demonstrated in clinical studies in animals. It is not approved for human use. |
| Enzyme Assay |
The in vitro antiprotozoal assay for Buparvaquone involves testing its activity against Theileria-infected cell cultures. The compound is serially diluted and added to the culture medium. After incubation, the number of infected cells or the parasite load is determined, and the IC50 is calculated from the dose-response curve.
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| Cell Assay |
In vitro cell culture studies for Buparvaquone utilize Theileria-infected bovine cells. Cells are treated with the compound, and cell viability is assessed. The parasite load is measured by qPCR or by microscopy. The compound's effect on the host cell and the parasite can be distinguished. Its mechanism of action on the mitochondrial electron transport chain can be studied.
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| Animal Protocol |
In vivo animal experiments for Buparvaquone are performed in cattle or other livestock infected with Theileria. The compound is administered by injection, and the animals are monitored for clinical signs of theileriosis. The parasite load in the blood is measured by qPCR or by microscopy. The efficacy of the treatment is assessed by the reduction in parasite load and the improvement in clinical signs.
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| ADME/Pharmacokinetics |
Buparvaquone has a molecular formula of C21H26O3 and a molecular weight of 326.43 g/mol. It is a solid compound that is soluble in organic solvents like DMSO. It is typically stored as a powder at room temperature for long-term stability. Its stability is maintained under recommended storage conditions. It is a yellow crystalline powder.
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| Toxicity/Toxicokinetics |
Toxicological data for Buparvaquone indicate that it is generally safe for use in veterinary medicine at therapeutic doses. However, it can cause local reactions at the injection site. As a hydroxynaphthoquinone, it has the potential for toxicity, and its use is restricted to veterinary applications. It is not approved for human use.
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| References |
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| Additional Infomation |
Buparvaquone is a veterinary drug approved for the treatment of theileriosis in cattle and other livestock. It is not approved for human use. It is an important tool for the control of this economically significant disease. Its mechanism of action as a mitochondrial electron transport inhibitor makes it a compound of interest for research into antiprotozoal agents.
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| Molecular Formula |
C21H26O3
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| Molecular Weight |
326.4293
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| Exact Mass |
326.188
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| CAS # |
88426-33-9
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| PubChem CID |
71768
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
460.7±45.0 °C at 760 mmHg
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| Melting Point |
178-184ºC
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| Flash Point |
246.5±25.2 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.574
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| LogP |
6.45
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
544
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NEGDTWQGGLJCTL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H26O3/c1-21(2,3)14-10-8-13(9-11-14)12-17-18(22)15-6-4-5-7-16(15)19(23)20(17)24/h4-7,13-14,22H,8-12H2,1-3H3
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| Chemical Name |
3-[(4-tert-butylcyclohexyl)methyl]-4-hydroxynaphthalene-1,2-dione
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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 |
| 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 : ~33.33 mg/mL (~102.10 mM)
DMF : 25 mg/mL (~76.59 mM) Ethanol : ~2 mg/mL (~6.13 mM) H2O : ~1 mg/mL (~3.06 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.66 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (7.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMF 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0634 mL | 15.3172 mL | 30.6344 mL | |
| 5 mM | 0.6127 mL | 3.0634 mL | 6.1269 mL | |
| 10 mM | 0.3063 mL | 1.5317 mL | 3.0634 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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