| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vivo |
In the digestive system, diloxide is hydrolyzed to produce its prodrug, diloxide furoate [1]. 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].
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| 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 |
| References |
[1]. DB08792
[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 (existing as Diloxanide furoate) is an antiprotozoal drug used to treat Entamoeba histolytica and other protozoan infections. Although not currently approved in the United States, a study by the Centers for Disease Control and Prevention (CDC) approved its use in treating 4,371 cases of Entamoeba histolytica infection between 1977 and 1990. Drug Indications Diloxanide can be used alone as a first-line treatment for asymptomatic (cyst-extruding) intestinal amebiasis caused by Entamoeba histolytica. Diloxanide can also be used in combination with or sequentially with other drugs (such as nitroimidazoles like metronidazole) to treat invasive or extraintestinal amebiasis. Mechanism of Action Not yet clear. Diloxanide may inhibit protein synthesis. Pharmacodynamics Diloxanide is an intestinal amebic bactericide, but its mechanism of action is not yet clear. Deloxalide destroys the trophozoites of Entamoeba histolytica, which eventually form cysts. Asymptomatic amoebic patients expel these cysts from their bodies. Deloxalide furate is a prodrug that hydrolyzes in the gastrointestinal tract to produce the active ingredient, deloxalide.
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| Molecular Formula |
C9H9CL2NO2
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|---|---|
| Molecular Weight |
234.0793
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| Exact Mass |
233.001
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| CAS # |
579-38-4
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| PubChem CID |
11367
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.439g/cm3
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| Boiling Point |
356.2ºC at 760 mmHg
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| Melting Point |
175°
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| Flash Point |
169.2ºC
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| Index of Refraction |
1.615
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| LogP |
2.158
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
203
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC(C(N(C1C=CC(OC(C2=CC=CO2)=O)=CC=1)C)=O)Cl
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| InChi Key |
GZZZSOOGQLOEOB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H9Cl2NO2/c1-12(9(14)8(10)11)6-2-4-7(13)5-3-6/h2-5,8,13H,1H3
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| Chemical Name |
2,2-dichloro-N-(4-hydroxyphenyl)-N-methylacetamide
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| Synonyms |
RD3803; RD-3803; RD 3803
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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 (~142.39 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.68 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 (10.68 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2720 mL | 21.3602 mL | 42.7204 mL | |
| 5 mM | 0.8544 mL | 4.2720 mL | 8.5441 mL | |
| 10 mM | 0.4272 mL | 2.1360 mL | 4.2720 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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