| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
As a luminal antiamoebic agent, Tiliquinol acts locally in the intestinal lumen to eliminate Entamoeba histolytica. Its mechanism of action likely involves chelation of metal ions essential for amoebic metabolism, similar to other 8-hydroxyquinoline derivatives, disrupting essential enzymatic processes in the parasite. Additionally, tiliquinol exhibits antibacterial activity against MRSA and its resistant biofilms through a dual-mechanism action, making it a compound of interest for drug repurposing studies.
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| ln Vitro |
In vitro studies have demonstrated that tiliquinol exhibits notable antibacterial activity against MRSA and its highly resistant biofilms, avoiding resistance occurrence. The combined antibacterial effects between tiliquinol and conventional antibiotics have been evaluated using the checkerboard dilution assay. As a non-absorbed anti-amoebic luminal agent, it is effective against Entamoeba infections. The compound is frequently employed in combination with tibroquinol for research on amoebic liver abscess.
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| ln Vivo |
In vivo, tiliquinol has been used successfully in combination with metronidazole and tiliquinol-tilbroquinol for the treatment of amebic liver abscess. As a non-absorbable luminal agent, it acts locally in the intestinal tract without significant systemic absorption. The tiliquinol-tilbroquinol combination has been used for the treatment of amoebic diseases. However, the combination agent was withdrawn from the market because of hepatotoxicity, limiting its clinical use.
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| Enzyme Assay |
For antimicrobial susceptibility testing, tiliquinol is evaluated using the checkerboard dilution assay. Overnight cultures of bacterial strains are prepared and serial dilutions of tiliquinol and conventional antibiotics are tested alone and in combination. Fractional inhibitory concentration indices (FICI) are calculated to determine synergistic, additive, or antagonistic interactions. For antiamoebic activity, Entamoeba histolytica cultures are used in standard susceptibility assays, with parasite viability assessed by microscopy or metabolic assays.
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| Cell Assay |
For cellular studies, relevant cell lines or microbial cultures are treated with tiliquinol at various concentrations. Antibacterial activity is assessed against MRSA and other bacterial strains using broth microdilution or agar diffusion methods. Biofilm inhibition is evaluated using crystal violet staining or confocal microscopy. For antiamoebic studies, Entamoeba histolytica trophozoites are cultured in appropriate media and treated with the compound, with parasite growth inhibition measured by counting or metabolic assays. Cytotoxicity is assessed in mammalian cell lines using MTT assays.
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| Animal Protocol |
For in vivo efficacy studies, animal models of amebic liver abscess are used. Tiliquinol is administered alone or in combination with tibroquinol. Efficacy is assessed by measuring parasite burden in liver tissues, survival rates, and histopathological analysis of liver lesions. For antibacterial studies, mouse models of MRSA infection are used to evaluate the compound's in vivo efficacy. However, the combination agent was withdrawn from the market because of hepatotoxicity, limiting clinical development.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of tiliquinol are characterized by its non-absorbable nature. Following oral administration, the compound remains in the intestinal lumen without significant systemic absorption, making it suitable for treating luminal infections. The compound has a density of 1.2±0.1 g/cm3 and a boiling point of 324.7±22.0 °C at 760 mmHg. It is typically administered orally for the treatment of intestinal amoebiasis. Comprehensive PK studies are limited due to the compound's withdrawal from the market.
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| Toxicity/Toxicokinetics |
Tiliquinol is a non-absorbed anti-amoebic luminal agent that was used in combination with tibroquinol. The combination agent was withdrawn from the market because of hepatotoxicity. Tiliquinol exhibits notable antibacterial activity against MRSA and its highly resistant biofilms, avoiding resistance occurrence. Due to its hepatotoxicity concerns, the compound is primarily used for research purposes rather than clinical applications. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
[1]. Nespola B, et al. First case of amebic liver abscess 22 years after the first occurrence. Parasite. 2015;22:20.
[2]. Desoubeaux G, et al. Unusual multiple large abscesses of the liver: interest of the radiological features and the real-time PCR to distinguish between bacterial and amebic etiologies. Pathog Glob Health. 2014;108(1):53-57. |
| Additional Infomation |
Tiliquinol is a hydroxyquinoline compound. It was previously used in combination with tebuproquinol, an antimicrobial drug. Due to hepatotoxicity, this combination formulation has been withdrawn from the market.
Tiliquinol is a non-absorbable antiamoebic agent with molecular formula C10H9NO and molecular weight 159.19. It is widely utilized in combination with tibroquinol for the research of amoebic liver abscess. The combination agent was withdrawn from the market because of hepatotoxicity. Tiliquinol also exhibits antibacterial activity against MRSA and its biofilms. It is for research use only and has not been approved for clinical applications. |
| Molecular Formula |
C10H9NO
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|---|---|
| Molecular Weight |
159.19
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| Exact Mass |
159.068
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| CAS # |
5541-67-3
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| PubChem CID |
71208
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
324.7±22.0 °C at 760 mmHg
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| Melting Point |
122-124°C
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| Flash Point |
150.2±22.3 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.666
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| LogP |
2.33
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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 |
0
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| Heavy Atom Count |
12
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| Complexity |
160
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1=C2N=CC=CC2=C(C)C=C1
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| InChi Key |
RPVGLMKJGQMQSN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H9NO/c1-7-4-5-9(12)10-8(7)3-2-6-11-10/h2-6,12H,1H3
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| Chemical Name |
5-methylquinolin-8-ol
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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 : 100 mg/mL (628.18 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (15.70 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 (15.70 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 | 6.2818 mL | 31.4090 mL | 62.8180 mL | |
| 5 mM | 1.2564 mL | 6.2818 mL | 12.5636 mL | |
| 10 mM | 0.6282 mL | 3.1409 mL | 6.2818 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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