| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Decoquinate acts as a competitive inhibitor at the quinol oxidation (Qo) site of cytochrome b, a key subunit of the cytochrome bc1 complex (mitochondrial complex III). By binding to this site, it blocks electron transfer from ubiquinol to cytochrome c, disrupting the proton motive force and subsequent ATP synthesis. This inhibition of the parasite's mitochondrial electron transport chain arrests energy metabolism, thereby halting parasite development and reproduction. Decoquinate specifically targets the sporozoite stage of Eimeria spp. and the first-generation schizonts, inhibiting both respiration and sporulation. It also acts on the liver and blood stages of Plasmodium. Importantly, decoquinate exhibits limited cross-resistance with atovaquone-resistant parasites, as molecular docking studies reveal distinctly different binding modes within the ubiquinol-binding site of cytochrome b.
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| ln Vitro |
In vitro, decoquinate exhibits single-digit nanomolar activity against blood-stage Plasmodium falciparum. It also shows low nanomolar activity against in vitro liver-stage P. yoelii. Against Neospora caninum tachyzoites in human foreskin fibroblasts, decoquinate demonstrates half-maximal proliferation inhibition (IC50) values ranging from 1.7 to 60 nM. In Toxoplasma gondii-infected fibroblasts, decoquinate shows potent antiparasitic effects. Importantly, when applied at concentrations of 5-10 μM, decoquinate does not affect the viability of host cells (human foreskin fibroblasts or splenocytes). It also exhibits significant anticoccidial activity by inhibiting the growth of Eimeria oocysts in the asexual reproduction stage.
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| ln Vivo |
In vivo, decoquinate has been extensively evaluated in livestock. In goats, dietary administration at doses of 0.3-4.0 mg/kg for 87 days effectively prevented clinical coccidiosis, with treated goats gaining significantly more weight and having fewer oocysts in feces compared to untreated controls. In poultry, decoquinate at 20-40 mg/kg effectively combats coccidiosis. In antimalarial studies, decoquinate provides partial causal prophylaxis when administered to P. yoelii-infected mice at 50 mg/kg. A single intramuscular dose of nanoparticle decoquinate (120 mg/kg) provided full causal prophylaxis in mice for 2-3 weeks. In pregnant neosporosis mouse models, oral decoquinate at 10 mg/kg/day for 5 days decreased fertility but failed to protect against cerebral infection.
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| Enzyme Assay |
Non-cellular assays for decoquinate focus on its inhibition of the mitochondrial bc1 complex. In a typical protocol, purified cytochrome bc1 complex is incubated with its substrate (ubiquinol) and varying concentrations of decoquinate. Enzyme activity is measured spectrophotometrically by monitoring the reduction of cytochrome c at 550 nm. The IC50 is calculated from the inhibition curve. Additionally, molecular docking studies can be performed to assess the binding mode of decoquinate within the ubiquinol-binding pocket of cytochrome b. Cell-free translation inhibition assays using parasite lysates can also confirm the compound's mechanism of action. These assays provide direct evidence of decoquinate's interaction with its molecular target without cellular interference.
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| Cell Assay |
Cellular assays for decoquinate employ various parasite culture systems. For antimalarial activity, P. falciparum-infected erythrocytes are cultured in 96-well plates and treated with serial dilutions of decoquinate (typically 0.1-100 nM) for 48-72 hours; parasite growth is measured by SYBR Green fluorescence or [³H]-hypoxanthine incorporation. For anticoccidial assays, Eimeria spp. oocysts are exposed to decoquinate and sporulation inhibition is assessed microscopically. For Neospora or Toxoplasma studies, human foreskin fibroblasts infected with tachyzoites are treated with decoquinate (0.1-10 μM) for 24-72 hours, and parasite proliferation is quantified by β-galactosidase assay or immunofluorescence. Host cell viability is assessed in parallel using MTT or resazurin assays to determine selectivity.
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| Animal Protocol |
In vivo animal experiments for decoquinate are primarily conducted in livestock and rodent models. In goats, a typical protocol involves assigning 50 animals to 5 groups receiving 0, 0.3, 0.5, 1.0, or 4.0 mg/kg decoquinate in feed for 87 days, with oral inoculation of 30,000 Eimeria oocysts on day 19; oocyst shedding, weight gain, and clinical signs are monitored. In antimalarial studies, mice are infected with P. berghei sporozoites and treated with single intramuscular doses of nanoparticle or microparticle decoquinate 2-8 weeks prior to infection; liver-stage efficacy is monitored by in vivo imaging. In poultry, decoquinate is administered in feed at 20-40 mg/kg, and efficacy is assessed by oocyst counts, intestinal lesion scoring, and weight gain.
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| ADME/Pharmacokinetics |
Decoquinate has poor pharmacokinetic properties due to its high lipophilicity and exceedingly poor aqueous solubility (0.06 μg/ml), rendering it difficult to administer. Following oral administration, it is incompletely absorbed. In rats, urinary excretion reaches a plateau after 2 days, corresponding to 6-12% of the administered dose. The highest tissue residues are found in liver and kidney. More than 96% of injected ¹⁴C-decoquinate is eliminated from blood within 1 hour. In mice, the elimination half-life of decoquinate is approximately 4.7-4.8 hours. Nanoformulations have been developed to improve bioavailability, with a nanosuspension achieving a 15-fold increase in bioavailability compared to standard formulations.
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| Toxicity/Toxicokinetics |
Decoquinate has a favorable toxicological profile. The acute oral LD50 in rats is >5000 mg/kg, with no deaths or overt signs of toxicity at this dose. It has low acute inhalational toxicity (4-hour LC50 >4190 mg/m³). Decoquinate is not irritating to the skin or eyes of rabbits and is not a skin sensitizer in guinea pigs. In repeated-dose studies, dogs were more sensitive than rats; the lowest NOEL was 15 mg/kg/day based on subdued behavior at 62.5 mg/kg/day. In rats, no treatment-related effects were observed in an 11-week oral gavage study. Decoquinate is not considered genotoxic based on weight-of-evidence from multiple Ames tests, and it is not likely to be a carcinogen. The EFSA concluded there is no appreciable risk to consumers' health from ingestion of decoquinate residues in animal tissues.
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| Additional Infomation |
Decoquinate is used in veterinary medicine to slow the growth and reproduction of coccidia parasites. It is an anticoccidial drug used in poultry. See also: Decoquinate; Monensin Sodium (ingredient); Bacitracin Zinc; Decoquinate (ingredient); Chlortetracycline; Decoquinate (ingredient)... See more...
Decoquinate is authorized as a feed additive under EU Council Directive 70/524/EEC for use in chickens, and is approved for the prevention and treatment of coccidiosis in calves and lambs. It is marketed under brand names such as Deccox®. The only anticoccidial medication approved for use in veal calves. Decoquinate has also demonstrated activity against Cryptosporidium parvum, Sarcocystis, and other apicomplexan parasites. Due to its poor aqueous solubility, nanoformulations and derivatives (e.g., quinoline O-carbamates RMB059 and RMB060) are being developed to improve bioavailability and enable human applications for malaria and other parasitic diseases. Research continues on its pharmaceutical potential beyond veterinary use. |
| Molecular Formula |
C24H35NO5
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|---|---|
| Molecular Weight |
417.54
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| Exact Mass |
417.251
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| CAS # |
18507-89-6
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| PubChem CID |
29112
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
517.9±45.0 °C at 760 mmHg
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| Melting Point |
86-87ºC
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| Flash Point |
267.0±28.7 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.541
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| LogP |
8.74
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
30
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| Complexity |
562
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C1C([H])=C2C(C(C(=O)OC([H])([H])C([H])([H])[H])=C([H])N([H])C2=C([H])C=1OC([H])([H])C([H])([H])[H])=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H]
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| InChi Key |
JHAYEQICABJSTP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H35NO5/c1-4-7-8-9-10-11-12-13-14-30-21-15-18-20(16-22(21)28-5-2)25-17-19(23(18)26)24(27)29-6-3/h15-17H,4-14H2,1-3H3,(H,25,26)
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| Chemical Name |
ethyl 6-decoxy-7-ethoxy-4-oxo-1H-quinoline-3-carboxylate
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| Synonyms |
Decoxy; Deccox; Decoquinate
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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 : ~1 mg/mL (~2.39 mM)
H2O : ~1 mg/mL (~2.39 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 | 2.3950 mL | 11.9749 mL | 23.9498 mL | |
| 5 mM | 0.4790 mL | 2.3950 mL | 4.7900 mL | |
| 10 mM | 0.2395 mL | 1.1975 mL | 2.3950 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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