| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Clofoctol targets the bacterial cell membrane, particularly disrupting its integrity, which leads to the inhibition of bacterial growth and viability. It is a membrane-active antibacterial agent that does not rely on inhibition of protein synthesis or cell wall synthesis for its antibacterial effect. The compound may also inhibit bacterial protein synthesis as a secondary mechanism. Its unique mechanism of action makes it effective against antibiotic-resistant strains.
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| ln Vitro |
Clofoctol (0-100 μM; 72 hours) Growth of sniper rifles [2]. Clofoctol in G1 phase (0–20 μM; 24 hours) [2]. ER is induced by clofoctol (0-30 μM; 0-24 hours). Translation is inhibited by trichlorophenol (0–40 μM; 24 hours) [2]. In Vero-81, trichlorophenol (0-100 μM; 24 h) exhibits antiviral properties against SARS-CoV-2. transition and start the UPR[2].
In vitro, Clofoctol demonstrates antibacterial activity against Gram-positive bacteria including Streptococcus pneumoniae and Staphylococcus aureus. The compound's membrane-active mechanism results in rapid bactericidal activity. It has been shown to be effective against antibiotic-resistant strains. Minimum inhibitory concentrations (MICs) for susceptible organisms are in the low microgram per milliliter range. Detailed in vitro susceptibility data are available from published studies. |
| ln Vivo |
In a human stent-carcinoma xenograft model, chlorphenol (175 mg/kg; intraperitoneal injection; once daily for 37 days) promotes tumor growth without causing toxicity [2]. In mice infected with SARS-CoV-2, pulmonary regulatory factors are decreased and SARS-CoV-2 replication is inhibited by chlorphenol (62.5 mg/kg; evident via intraperitoneal injection; twofold) [3].
In vivo, Clofoctol has demonstrated efficacy in managing respiratory tract infections such as pneumonia and bronchitis. It is effective against Gram-positive bacterial infections in the respiratory tract. The compound has been used clinically for the treatment of respiratory infections. Its membrane-active mechanism provides rapid bactericidal activity, making it effective for the treatment of acute infections. |
| Enzyme Assay |
In vitro susceptibility testing for antibiotics typically uses broth microdilution or agar dilution methods according to CLSI guidelines. Bacterial cultures are prepared at a standardized inoculum and incubated with varying concentrations of Clofoctol in 96-well plates or on agar plates. Minimum inhibitory concentrations (MICs) are determined as the lowest concentration that inhibits visible bacterial growth after 18-24 hours of incubation. Time-kill assays are performed to assess bactericidal activity.
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| Cell Assay |
Cell viability assay [2]
Cell Types: Prostate cancer Cell Types: LNCaP, DU145, PC3, LAPC4, CWR22Rv1 and C42B Tested Concentrations: In 0- and Vero-81-TMPRSS2 cells, the IC50 was 9.3 μM and 11.59 μM, respectively [3]. 100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited cell growth with IC50 values ranging from 10 to 15 μM. Cell viability assay[2] Cell Types: PC3 Tested Concentrations: 0, 10 and 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of G1 arrest. RT-PCR[2] Cell Types: PC3 Tested Concentrations: 0, 5, 10, 15, 20 and 30 μM Incubation Duration: 24 hrs (hours) Experimental Results: Splicing of XBP-1 mRNA increased in PC3 cells in a dose-dependent manner. PstI digestion products of XBP-1 mRNA were diminished in a dose-dependent manner. Western Blot Analysis[2] Cell Types: PC3 Tested Concentrations: 0, 5, 10, 15, 20, 25 and 30 μM Incubation Duration: 0, 0.5, 1, 3, 6 and 9 hrs (hours) or 24 hrs (hours) (cell cycle) Experimental Results: Phosphorylated eIF2α levels increased in a dose- and time-dependent manner, upregulated CHOP expression, and increased BiP expressi Cellular assays for membrane-active antibiotics typically use bacterial cell cultures. Bacteria are treated with varying concentrations of Clofoctol, and cell viability is assessed by colony counting or using vital dyes. Membrane integrity is assessed using fluorescent dyes such as propidium iodide or SYTOX Green, which enter cells with compromised membranes. Membrane potential is measured using fluorescent probes such as DiSC₃(5). |
| Animal Protocol |
Animal/Disease Models: 4-year-old male athymic nude mice (BALB/c, nu/nu-NCr) for 6 weeks, human prostate cancer xenograft model [2]
Doses: 175 mg/kg Route of Administration: intraperitoneal (ip) injection, one time/day, Result lasting 37 days: Dramatically inhibited PC3 tumor growth and diminished tumor weight by 60%. Animal/Disease Models: K18-hACE2 transgenic C57BL/6J mice infected with SARS-CoV-2 [3] Doses: 62.5 mg/kg Route of Administration: intraperitoneal (ip) injection 1 hour and 8 hrs (hrs (hours)) after infection Experimental Results: Induced weight loss and diminished virus in the body Loading lungs. The expression of transcripts encoding IL-6, TNFα, IL12p40, IFNβ, IFNγ and the interferon-stimulated genes (ISGs) Mx1, Ifi44 and ISG15 was Dramatically diminished. Animal/Disease Models: 8-10 weeks old female C57BL/6J mice [3] Doses: 62.5mg/kg Route of Administration: intraperitoneal (ip) injection, once (pharmacokinetic/PK/PKs) Experimental Results: The lung concentration reached 61μM, and the drug was administered within almost 24 hrs (hrs (hours)). Stay above this level for 4 hrs (hrs (hours)) to In vivo animal studies for respiratory tract infections typically use mouse or rat models of pneumonia or bronchitis induced by intranasal inoculation of Streptococcus pneumoniae or Staphylococcus aureus. Animals are administered Clofoctol orally or parenterally at various doses, and bacterial load in the lungs is determined by CFU counting. Survival is monitored as an endpoint. Inflammatory markers and histopathology are also assessed. |
| ADME/Pharmacokinetics |
Clofoctol is administered orally for the treatment of respiratory tract infections. It is well-absorbed following oral administration and distributes to the respiratory tract where it exerts its antibacterial effect. The compound is metabolized in the liver, and its metabolites are excreted via the kidneys and bile. The compound has a favorable PK profile for the treatment of respiratory infections, with good lung penetration.
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| Toxicity/Toxicokinetics |
Clofoctol has a favorable safety profile, with an oral LD50 in male rats of >4 g/kg. The compound is generally well-tolerated at therapeutic doses. Common side effects may include gastrointestinal disturbances. Serious adverse effects are rare. The compound has been used clinically for the treatment of respiratory infections, and its safety profile is well-established.
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| References |
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| Additional Infomation |
2-[(2,4-dichlorophenyl)methyl]-4-(2,4,4-trimethylpentane-2-yl)phenol is a diarylmethane compound. Chlorfort is an antibacterial antibiotic active against Gram-positive bacteria. Chlorfort is used to treat upper and lower respiratory tract infections.
Clofoctol (octofene) is a synthetic phenol derivative antibiotic used for the treatment of respiratory tract infections caused by Gram-positive bacteria. It acts as a membrane-active antibacterial agent, disrupting bacterial cell membrane integrity. The compound has demonstrated efficacy in managing pneumonia and bronchitis. It is effective against antibiotic-resistant strains and has a favorable safety profile with an oral LD50 >4 g/kg in rats. Clofoctol is available for research use. |
| Molecular Formula |
C21H26OCL2
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|---|---|
| Molecular Weight |
365.33654
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| Exact Mass |
364.136
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| CAS # |
37693-01-9
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| Related CAS # |
37693-01-9;
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| PubChem CID |
2799
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| Appearance |
White to off-white solid powder
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| Density |
1.127 g/cm3
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| Boiling Point |
447.7ºC at 760 mmHg
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| Melting Point |
78°
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| Flash Point |
160.4ºC
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| Index of Refraction |
1.555
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| LogP |
7.003
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
401
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HQVZOORKDNCGCK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H26Cl2O/c1-20(2,3)13-21(4,5)16-7-9-19(24)15(11-16)10-14-6-8-17(22)12-18(14)23/h6-9,11-12,24H,10,13H2,1-5H3
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| Chemical Name |
2-[(2,4-dichlorophenyl)methyl]-4-(2,4,4-trimethylpentan-2-yl)phenol
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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 (~273.72 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.84 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 (6.84 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.84 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 | 2.7372 mL | 13.6859 mL | 27.3718 mL | |
| 5 mM | 0.5474 mL | 2.7372 mL | 5.4744 mL | |
| 10 mM | 0.2737 mL | 1.3686 mL | 2.7372 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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