| Size | Price | Stock | Qty |
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| 5mg |
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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 |
Tribendimidine targets L-type nicotinic acetylcholine receptors (nAChRs) in parasitic nematodes. By acting as an agonist at these receptors, it causes spastic paralysis of the worms, leading to their expulsion from the host. This mechanism is similar to that of other anthelmintics such as pyrantel and levamisole. The compound's broad-spectrum activity against soil-transmitted helminths makes it a valuable tool for the treatment of parasitic infections.
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| ln Vitro |
C exhibits intoxication with 100 μg/mL of trimethidine for a 24-hour period. elegans [3]. With an LC50 value of 54.4 μg/mL, which indicates the concentration at which half of the animals die, triphenyldiamidine (0-100 μg/mL; 6 days) exhibits toxicity [3]. Levoamisole-resistant mutants are resistant to tribendimidine, while trb mutant hermaphrodites are resistant to infertility produced by tribendimidine (0-200 μg/mL; 64 h). [3].
In vitro, Tribendimidine induces mortality in newly excysted Opisthorchis felineus metacercariae and adult flukes with IC50s of 0.23 µM and 0.19 µM, respectively. These data confirm its potent anthelmintic activity. The compound's activity against nematodes is mediated through L-type nAChR agonism. It is effective against a broad range of parasitic worms. |
| ln Vivo |
Tribendimidine (75 and 150 mg/kg; oral; one time) has demonstrated C-inhibitory action. sinensis against O and in rats. 400 mg/kg of viverrini in hamsters [2].
In vivo, Tribendimidine is orally active and has been used in clinical studies for the treatment of intestinal helminth infections. It is particularly effective against A. lumbricoides and N. americanus. The compound has been evaluated in clinical trials and has shown high cure rates. It is a promising alternative to existing anthelmintics for the treatment of soil-transmitted helminthiasis. |
| Enzyme Assay |
In vitro anthelmintic assays are performed to evaluate Tribendimidine's activity against parasitic worms. Worms (e.g., newly excysted metacercariae or adult flukes) are incubated with varying concentrations of the compound. Worm mortality is assessed, and IC50 values are determined. For nematodes, motility assays are used to assess the effects of the compound on worm movement. These assays confirm the compound's anthelmintic activity and potency.
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| Cell Assay |
In vitro cell-based assays for Tribendimidine are not typically performed, as the compound's primary target is parasitic worms. However, studies on L-type nAChR activation can be conducted using cells expressing the receptor. Calcium flux or electrophysiological assays can measure the compound's agonistic activity at the receptor. These assays characterize the compound's mechanism of action.
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| Animal Protocol |
Animal/Disease Models: C. sinensis infected female Wistar rats [2]
Doses: 75 mg/kg and 150 mg/kg Route of Administration: Orally once. Experimental Results: 99.1% reduction in worm load at 150 mg/kg and 99.1% reduction in worm load at 75 mg /kg dose, the reduction remained significant (68.9%). In vivo animal experiments with Tribendimidine are conducted in animal models of parasitic infection. Rodents infected with helminths are treated with the compound orally, and worm burden is assessed by counting worms in the intestines after necropsy. Efficacy is measured by the reduction in worm count compared to untreated controls. These studies confirm the compound's in vivo efficacy and are used to determine optimal dosing regimens. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Tribendimidine include oral activity. The compound has a molecular formula of C28H32N6 and a molecular weight of 452.59. It is a solid. Storage: refrigerated (0-10°C), under inert gas. Specific PK parameters such as half-life, Cmax, and bioavailability are not detailed in the available literature.
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| Toxicity/Toxicokinetics |
Safety and toxicology data for Tribendimidine are available from clinical studies. The compound is generally well-tolerated, with mild and transient adverse effects reported. Common adverse effects may include abdominal pain, nausea, and headache. The compound is for research use and for approved clinical applications; not for over-the-counter use. Standard safety precautions apply.
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| References |
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| Additional Infomation |
Tribendimidine has CAS number 115103-15-6, molecular formula C28H32N6, and molecular weight 452.59. It is an orally active, broad-spectrum anthelmintic agent. It is highly effective against A. lumbricoides and N. americanus. It is an L-type nAChR agonist. Purity: ≥99%. Not for over-the-counter use; for prescription and research applications.
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| Molecular Formula |
C28H32N6
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|---|---|
| Molecular Weight |
452.59388
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| Exact Mass |
452.269
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| Elemental Analysis |
C, 74.30; H, 7.13; N, 18.57
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| CAS # |
115103-15-6
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| PubChem CID |
3086564
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.04g/cm3
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| Boiling Point |
618.2ºC at 760mmHg
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| Flash Point |
327.7ºC
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| Vapour Pressure |
3.26E-15mmHg at 25°C
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| Index of Refraction |
1.575
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| LogP |
6.41
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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 |
8
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| Heavy Atom Count |
34
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| Complexity |
651
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(/C(=N/C1C=CC(/N=C/C2C=CC(/C=N/C3C=CC(/N=C(/N(C)C)\C)=CC=3)=CC=2)=CC=1)/C)C
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| InChi Key |
XOIOGKHKNQYULW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H32N6/c1-21(33(3)4)31-27-15-11-25(12-16-27)29-19-23-7-9-24(10-8-23)20-30-26-13-17-28(18-14-26)32-22(2)34(5)6/h7-20H,1-6H3
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| Chemical Name |
N'-[4-[[4-[[4-[1-(dimethylamino)ethylideneamino]phenyl]iminomethyl]phenyl]methylideneamino]phenyl]-N,N-dimethylethanimidamide
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| Synonyms |
Tribendimidine
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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 (~110.48 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.52 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 (5.52 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 | 2.2095 mL | 11.0475 mL | 22.0951 mL | |
| 5 mM | 0.4419 mL | 2.2095 mL | 4.4190 mL | |
| 10 mM | 0.2210 mL | 1.1048 mL | 2.2095 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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