| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
Diloxanide furoate is a prodrug that is hydrolyzed to the active parent compound, diloxanide, in the intestine. It acts as an amebicide, effective against trophozoites in the intestinal tract. It may inhibit protein synthesis.
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| ln Vitro |
The MIC values of diloxanide furoate (1.95-2.5 μg/ml) are 2.5 μg/ml, 2.5 μg/ml, and 1.95 μg/ml, respectively, and it has strong action against various strains of Entamoeba histolytica, BYso (bacteria-growing), SFL3 (growing with Chrithidia sp.), and SFL3 (growing axenically).
In vitro, diloxanide furoate is hydrolyzed to diloxanide, which is active against Entamoeba histolytica. It is effective against trophozoites. Its activity has been characterized in various in vitro assays. |
| ln Vivo |
Different dosages of diloxanide furoate (oral; 75-200 mg/kg; 3 days; once daily) have been found to be beneficial in weaned rats. All treated rats recovered at the 200 mg/kg dose, and no amoebic lesions were seen in the cecum. Furthermore, the cure rates of rats in the therapy group were 85%, 77%, and 44.4% at dosages of 150 mg/kg, 100 mg/kg, and 75 mg/kg, respectively. This drug's ED50 value in rats is 77.9 mg/kg[2].
In vivo, diloxanide furoate is used as a primary agent in the treatment of asymptomatic (cyst passers) intestinal amebiasis caused by Entamoeba histolytica. In mild or asymptomatic infections, cures of 83 to 95% have been achieved. It is not effective against extraintestinal amebiasis. |
| Enzyme Assay |
In vitro susceptibility testing for diloxanide furoate involves culturing Entamoeba histolytica trophozoites with the compound. The prodrug is hydrolyzed to the active diloxanide. Parasite viability is assessed by microscopy or metabolic assays. MICs are determined.
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| Cell Assay |
Cell-based assays for diloxanide furoate involve treating Entamoeba histolytica cultures with the compound and measuring parasite growth inhibition. The compound's ability to kill trophozoites is assessed.
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| Animal Protocol |
Animal/Disease Models: Weaned Wistar rats [2]
Doses: 200 mg/kg; 150 mg/kg; 100 mg/kg; 75 mg/kg Route of Administration: oral; 75-200 mg/kg; 3 days; results one time/day Experimental Results: Can fight against intestinal (caecum) amoebiasis in rats. In vivo animal studies for diloxanide furoate are limited. Efficacy in animal models of amebiasis has been demonstrated. The compound's ability to eliminate cysts from the intestinal lumen is assessed. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Bioavailability is 90% (in the form of dicoxabinib injection), but dicoxabinib furoate is slowly absorbed in the gastrointestinal tract. Renal excretion (90%, rapidly excreted as glucuronide metabolites). 10% is excreted in feces as dicoxabinib. Metabolism/Metabolites Hydrolysis produces furanoic acid and dicoxabinib, the latter undergoing extensive glucuronidation (99% of dicoxabinib exists in systemic circulation as glucuronide, 1% exists as free dicoxabinib). Biological Half-Life 3 hours Pharmacokinetic properties of diloxanide furoate are characterized by its poor systemic absorption. The prodrug is hydrolyzed to diloxanide in the intestine. The active compound acts locally in the intestinal lumen. It is excreted in the feces. |
| Toxicity/Toxicokinetics |
Diloxanide furoate is generally well-tolerated. Common side effects include flatulence, nausea, and diarrhea. It is contraindicated in patients with known hypersensitivity. It has a favorable safety profile.
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| References |
[1]. VA CLASSIFICATION. Diloxanide (Systemic)
[2]. D K Chatterjee, et al. Antiamoebic activity of chonemorphine, a steroidal alkaloid, in experimental models. Parasitol Res. 1987;74(1):30-3. |
| Additional Infomation |
Diloxanide is a carboxylic acid ester formed by the condensation of the carboxyl group of furan-2-carboxylic acid and the hydroxyl group of 2,2-dichloro-N-(4-hydroxyphenyl)-N-methylacetamide. It is a drug used to treat asymptomatic amebiasis. It is both an anti-amoebic drug and a prodrug. It belongs to the furan class, carboxylic acid ester class, tertiary amide class, and organochlorine class. Drug Indications Diloxanide is used alone as a first-line drug for the treatment of asymptomatic (cyst-extruded) intestinal amebiasis caused by Entamoeba histolytica. Diloxacillin can also be used concurrently or sequentially with other drugs (such as nitroimidazoles like metronidazole) to treat invasive or extraintestinal amebiasis. Mechanism of Action Diloxacillin is not yet clear. Diloxacillin may inhibit protein synthesis.
Diloxanide furoate (Furamide) is an amebicide used to treat infection with amoebas. It is a prodrug of diloxanide. It is used as a primary agent in the treatment of asymptomatic intestinal amebiasis caused by Entamoeba histolytica. It is not effective against extraintestinal amebiasis. |
| Molecular Formula |
C14H11CL2NO4
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|---|---|
| Molecular Weight |
328.15
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| Exact Mass |
327.007
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| CAS # |
3736-81-0
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| PubChem CID |
19529
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.265
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
21
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| Complexity |
383
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CC=CO1)OC2=CC=C(N(C(C(Cl)Cl)=O)C)C=C2
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| InChi Key |
BDYYDXJSHYEDGB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H11Cl2NO4/c1-17(13(18)12(15)16)9-4-6-10(7-5-9)21-14(19)11-3-2-8-20-11/h2-8,12H,1H3
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| Chemical Name |
[4-[(2,2-dichloroacetyl)-methylamino]phenyl] furan-2-carboxylate
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| Synonyms |
Histomibal; Amebiazol; Diloxanide furoate
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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 : ≥ 50 mg/mL (~152.37 mM)
Ethanol : ~20 mg/mL (~60.95 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.62 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 (7.62 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 (7.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 | 3.0474 mL | 15.2369 mL | 30.4739 mL | |
| 5 mM | 0.6095 mL | 3.0474 mL | 6.0948 mL | |
| 10 mM | 0.3047 mL | 1.5237 mL | 3.0474 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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