| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
| 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).
|
|---|---|
| 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].
|
| 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. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Bioavailability is 90% (in diloxanide parental form), however diloxanide furoate is slowly absorbed from the gastrointestinal tract. Renal (90%, rapidly excreted as glucuronide metabolite). 10% is excreted in the feces as diloxanide. Metabolism / Metabolites Hydrolyzed to furoic acid and diloxanide, which undergoes extensive glucuronidation (99% of diloxanide occurs as glucuronide and 1% as free diloxanide in the systemic circulation). Biological Half-Life 3 hours |
| 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 furoate is a carboxylic ester resulting from the formal condensation of the carboxy group of furan-2-carboxylic acid with the hydroxy group of 2,2-dichloro-N-(4-hydroxyphenyl)-N-methylacetamide. It is a drug used for the treatment of asymptomatic amebiasis. It has a role as an antiamoebic agent and a prodrug. It is a member of furans, a carboxylic ester, a tertiary carboxamide and an organochlorine compound.
Drug Indication Diloxanide is used alone as a primary agent in the treatment of asymptomatic (cyst passers) intestinal amebiasis caused by Entamoeba histolytica. Diloxanide may also be used concurrently, or sequentially, with other agents such as the nitroimidazoles (eg. metronidazole) in the treatment of invasive or extraintestinal forms of amebiasis. Mechanism of Action Unknown. Diloxanide may inhibit protein synthesis. |
| Molecular Formula |
C14H11CL2NO4
|
|---|---|
| Molecular Weight |
328.15
|
| Exact Mass |
327.007
|
| CAS # |
3736-81-0
|
| PubChem CID |
19529
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
3.265
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
21
|
| Complexity |
383
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=CC=CO1)OC2=CC=C(N(C(C(Cl)Cl)=O)C)C=C2
|
| InChi Key |
BDYYDXJSHYEDGB-UHFFFAOYSA-N
|
| 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
|
| Chemical Name |
[4-[(2,2-dichloroacetyl)-methylamino]phenyl] furan-2-carboxylate
|
| Synonyms |
Histomibal; Amebiazol; Diloxanide furoate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~152.37 mM)
Ethanol : ~20 mg/mL (~60.95 mM) |
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
