| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
Niclofolan targets the metabolic pathways of parasitic worms, disrupting their energy production and leading to their elimination. As an anthelmintic, it interferes with parasite metabolism, likely affecting mitochondrial function or energy metabolism in helminths. The compound is a polychlorinated biphenyl (PCB) derivative and is intended for use as an insecticide. Its precise molecular target in parasites is not fully characterized in publicly available sources.
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| ln Vitro |
The effectiveness of niclofolan (0.12 mg/mL, 60 minutes) against Gyrodactylus sp. in vitro circumstances [3].
In vitro, Niclofolan has been tested against various parasites in culture systems. It demonstrates anthelmintic activity against helminths, inhibiting their growth and survival. The compound's activity is assessed by measuring parasite motility, viability, or metabolic activity. Detailed in vitro data are available in veterinary parasitology literature. The compound is used as a reference anthelmintic in some studies. |
| ln Vivo |
Sheep with Fasciola hepatica infection respond well to intramuscular injections of chlorofluran (2 mg/kg) [2]. For rats infected with Plasmodium elodea, clofolan (1 or 2 mg/kg, orally administered by gavage) had a therapeutic effect [4].
In vivo, Niclofolan is administered orally to livestock for the treatment of parasitic infections. It is effective against gastrointestinal and hepatic helminths. The compound is used in veterinary medicine for the control of parasitic diseases in animals. Detailed in vivo efficacy data and dosing regimens are available in veterinary pharmacology literature. The compound is not used in human medicine. |
| Enzyme Assay |
In vitro anthelmintic assays for Niclofolan typically involve culturing parasites (e.g., Fasciola hepatica or other trematodes) in medium containing varying concentrations of the compound (0.1-100 μg/mL). Parasite motility is assessed microscopically at various time points (1-72 hours). Viability is confirmed by lack of movement upon stimulation or by vital dye exclusion. IC₅₀ values are calculated from dose-response curves. Controls include vehicle and known anthelmintics (e.g., triclabendazole). Assays are performed at 37°C with appropriate culture conditions for each parasite species.
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| Cell Assay |
Cell viability assay [3]
Cell Types: Gyrodactylus sp. (parasite) Tested Concentrations: 0.12 mg/mL Incubation Duration: 60 minutes Experimental Results: The number of viable Gyrodactylus sp is diminished. 100%. Cell-based studies for Niclofolan are limited, as the compound is primarily used in veterinary parasitology. In vitro cytotoxicity may be assessed using mammalian cell lines (e.g., HepG2 or primary hepatocytes) to evaluate safety. Cells are cultured in DMEM with 10% FBS and treated with Niclofolan at various concentrations for 24-72 hours. Cell viability is assessed by MTT or LDH release assays. IC₅₀ values for cytotoxicity are calculated. Selectivity index (antiparasitic IC₅₀ / cytotoxic IC₅₀) is determined. |
| Animal Protocol |
Animal/Disease Models: Fasciola hepatica-infected sheep [2]
Doses: 2 mg/kg Route of Administration: intramuscularinjection Experimental Results: demonstrated effectiveness against infection, and produced no adverse reactions except for transient pain symptoms at the injection site. Animal/Disease Models: Rats infected with P.iloktsuenesis [4] Doses: 1 mg/kg, one time/day, for 3 days; 2 mg/kg, once every other day, 2 times in a row. Route of Administration: po (oral gavage). Experimental Results: Reduction of worms in rats. In vivo, Niclofolan is typically administered orally to livestock (e.g., cattle, sheep, pigs) at doses specified in veterinary formularies. The compound may be given as a single dose or as part of a treatment regimen. Efficacy is assessed by fecal egg count reduction tests or by post-mortem worm counts. Safety is monitored by clinical observation and blood chemistry. The compound is used in veterinary practice under appropriate regulatory oversight. All procedures follow veterinary guidelines. |
| ADME/Pharmacokinetics |
Niclofolan (C₁₂H₆Cl₂N₂O₆, MW ~345) is a water-insoluble, lipophilic compound. It is orally bioavailable in animals. The compound is metabolized and excreted in animals. Detailed pharmacokinetic parameters are available in veterinary pharmacology literature. The compound's half-life and tissue residues are relevant for food safety considerations in livestock.
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| Toxicity/Toxicokinetics |
Niclofolan has been used in veterinary medicine and has undergone toxicological evaluation for use in food-producing animals. The compound's safety profile includes considerations of tissue residues and withdrawal times. At therapeutic doses, it is generally well-tolerated in livestock. Overdose may cause toxicity. The compound is not approved for human use. Standard veterinary safety precautions should be followed.
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| References |
[1]. T Eckhardt, Treatment of human fascioliasis with niclofolan. Gastroenterology. 1981 Oct; 81(4):795-8.
[2]. B H Ali, T Hassan, et al. The effect of niclofolan on desert sheep experimentally infected with immature Fasciola gigantica. J Vet Pharmacol Ther. 1985 Dec;8(4):398-403. [3]. Santamarina M. T., et al. Anthelmintic treatment against Gyrodactylus sp. infecting rainbow trout Oncorhynchus mykiss. Diseases of Aquatic Organisms, 1991 10(1): 39-43. [4]. Rim H J, et al. Expermental chemotherapeutic effects of niclofolan (Bayer 9015, Bilevon) on the animals infected with Paragonimus westermani or P. iloktsuenensis. The Korean Journal of Parasitology, 1976, 14(2): 140-146. |
| Additional Infomation |
Niclofolan is a polychlorinated biphenyl (PCB). It is intended for use as an insecticide. Synonyms: Dettol; bile acids; Bay 9015.
Niclofolan is a veterinary anthelmintic used for the treatment of parasitic infections in livestock. Its primary applications include control of liver flukes and other trematodes. The compound is not approved for human use. It is available from veterinary pharmaceutical suppliers. Its use is regulated in many countries due to food safety concerns. The compound is for research and veterinary use only. |
| Molecular Formula |
C12H6CL2N2O6
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|---|---|
| Molecular Weight |
345.088
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| Exact Mass |
343.96
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| CAS # |
10331-57-4
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| PubChem CID |
5284586
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
424.9±45.0 °C at 760 mmHg
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| Flash Point |
210.8±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.706
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| LogP |
3.97
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
22
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| Complexity |
402
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=C(C=C(C(=C1C2=C(C(=CC(=C2)Cl)[N+](=O)[O-])O)O)[N+](=O)[O-])Cl
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| InChi Key |
XULACPAEUUWKFX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H6Cl2N2O6/c13-5-1-7(11(17)9(3-5)15(19)20)8-2-6(14)4-10(12(8)18)16(21)22/h1-4,17-18H
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| Chemical Name |
4-chloro-2-(5-chloro-2-hydroxy-3-nitrophenyl)-6-nitrophenol
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| Synonyms |
Niclofolano; Niclofolan; Menichlopholan
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.8978 mL | 14.4890 mL | 28.9779 mL | |
| 5 mM | 0.5796 mL | 2.8978 mL | 5.7956 mL | |
| 10 mM | 0.2898 mL | 1.4489 mL | 2.8978 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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