Clofoctol
Based on 1 publication(s) in Google Scholar
Clofoctol is a bacteriostatic antibiotic. Clofoctol is used in the treatment of respiratory tract and ear, nose and throat infections caused by Gram-positive bacteria. Clofoctol is only functional against Gram-positive bacteria and can penetrate into human lung tissue. Clofoctol is also an inhibitor of prostate cancer. Clofoctol has antiviral potency.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.97%
- No. CAS: 37693-01-9
- Fòrmula: C21H26Cl2O
- Peso molecular:365.34
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Clofoctol
MoreVer todos los productos específicos de isoformas Antibiotic
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Actividad biológica
Clofoctol (0-100 μM; 72 h) inhibits prostate cancer cell growth[2].
Clofoctol (0-20 μM; 24 h) arrests cell cycle at G1 phase[2].
Clofoctol (0-30 μM; 0-24 h) induces ER stress and activates UPR pathways[2].
Clofoctol (0-40 μM; 24 h) inhibits translation[2].
Clofoctol (0-100 μM; 24 h) shows antiviral effect against SARS-CoV-2 with IC50s of 9.3 μM and 11.59 μM in Vero-81 and Vero-81-TMPRSS2 cells, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Prostate cancer cell lines: LNCaP, DU145, PC3, LAPC4, CWR22Rv1 and C42B
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Concentration:0-100 μM
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Incubation Time:72 h
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Result:Inhibited cell growth with IC50 values ranging from 10 to 15 μM.
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Cell Line:PC3
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Concentration:0, 10 and 20 μM
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Incubation Time:24 h
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Result:Induced a G1 arrest.
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Cell Line:PC3
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Concentration:0, 5, 10, 15, 20 and 30 μM
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Incubation Time:24 h
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Result:Increased the splicing of XBP-1 mRNA in PC3 cells in a dose-dependent manner. Dose-dependently decreased PstI digestion products from XBP-1 mRNA.
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Cell Line:PC3
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Concentration:0, 5, 10, 15, 20, 25 and 30 μM
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Incubation Time:0, 0.5, 1, 3, 6 and 9 h or 24 h (cell cycle)
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Result:Dose- and time-dependently increased the level of phosphorylated eIF2α, up-regulated CHOP expression, and increased the expression of BiP.
Led to a dose-dependent decrease in the levels of cyclin A and cyclin D1.
Clofoctol (62.5 mg/kg; i.p.; twice) inhibits SARS-CoV-2 replication and lowers inflammation in lungs in mice with SARS-CoV-2 infection[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male athymic nude mice (BALB/c, nu/nu-NCr) aged 4–6 weeks, human prostate cancer xenograft model[2]
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Dosage:175 mg/kg
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Administration:Intraperitoneal injection, daily for 37 days
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Result:Significantly inhibited PC3 tumour growth, tumour weight was also reduced by 60%.
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Animal Model:K18-hACE2 transgenic C57BL/6J mice with SARS-CoV-2 infection[3]
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Dosage:62.5 mg/kg
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Administration:Intraperitoneal injection, 1h and 8h post-infection
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Result:Induced body weight loss, reduced the viral load in the lungs. The expression of transcripts encoding IL-6, TNFα, IL12p40, IFNβ, IFNγ and the interferon-stimulated genes (ISG) Mx1, Ifi44 and ISG15 was markedly reduced.
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Animal Model:8–10 week-old female C57BL/6J mice[3]
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Dosage:62.5mg/kg
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Administration:Intraperitoneal injection, once (Pharmacokinetics)
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Result:Reached concentrations up to 61 μM in the lungs and remained above this level for almost 4h as early as 30 min after injection.
Chemical Information
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No. CAS 37693-01-9
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Appearance Solid
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Peso molecular 365.34
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Fòrmula C21H26Cl2O
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Color White to off-white
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SMILES
OC1=CC=C(C(C)(C)CC(C)(C)C)C=C1CC2=CC=C(Cl)C=C2Cl
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Initial Source
Bacillus subtilis
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Drug Deliv Transl Res
Leveraging quantum chemical properties in transfer learning for predicting blood-brain barrier permeability of drugs. [Abstract]2025 Oct 29. PMID: 41160380
Solvente y solubilidad
DMSO : 100 mg/mL (273.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.84 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ghilardi PL, et al. Treatment of ear, nose and throat infections with clofoctol. Drugs Exp Clin Res. 1985;11(11):815-8. [Content Brief]
[2]. Wang M, et al. Identification of an old antibiotic clofoctol as a novel activator of unfolded protein response pathways and an inhibitor of prostate cancer. Br J Pharmacol. 2014 Oct;171(19):4478-89. [Content Brief]
[3]. Belouzard S, et al. Clofoctol inhibits SARS-CoV-2 replication and reduces lung pathology in mice. PLoS Pathog. 2022 May 19;18(5):e1010498. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7372 mL | 13.6859 mL | 27.3718 mL | 68.4294 mL |
| 5 mM | 0.5474 mL | 2.7372 mL | 5.4744 mL | 13.6859 mL | |
| 10 mM | 0.2737 mL | 1.3686 mL | 2.7372 mL | 6.8429 mL | |
| 15 mM | 0.1825 mL | 0.9124 mL | 1.8248 mL | 4.5620 mL | |
| 20 mM | 0.1369 mL | 0.6843 mL | 1.3686 mL | 3.4215 mL | |
| 25 mM | 0.1095 mL | 0.5474 mL | 1.0949 mL | 2.7372 mL | |
| 30 mM | 0.0912 mL | 0.4562 mL | 0.9124 mL | 2.2810 mL | |
| 40 mM | 0.0684 mL | 0.3421 mL | 0.6843 mL | 1.7107 mL | |
| 50 mM | 0.0547 mL | 0.2737 mL | 0.5474 mL | 1.3686 mL | |
| 60 mM | 0.0456 mL | 0.2281 mL | 0.4562 mL | 1.1405 mL | |
| 80 mM | 0.0342 mL | 0.1711 mL | 0.3421 mL | 0.8554 mL | |
| 100 mM | 0.0274 mL | 0.1369 mL | 0.2737 mL | 0.6843 mL |
Clofoctol Related Classifications
HY-B1150 Related Classifications
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