Clofoctol

Cat. No.: HY-B1150 Purity: 99.75%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Clofoctol Chemical Structure

CAS No. : 37693-01-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 99	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 99	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
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5 g		Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

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.

Cell Viability Assay^[2]

Cell Line:	Prostate cancer cell lines: LNCaP, DU145, PC3, LAPC4, CWR22Rv1 and C42B
Concentration:	0-100 μM
Incubation Time:	72 h
Result:	Inhibited cell growth with IC₅₀ values ranging from 10 to 15 μM.

Cell Viability Assay^[2]

Cell Line:	PC3
Concentration:	0, 10 and 20 μM
Incubation Time:	24 h
Result:	Induced a G₁ arrest.

RT-PCR^[2]

Cell Line:	PC3
Concentration:	0, 5, 10, 15, 20 and 30 μM
Incubation Time:	24 h
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.

Western Blot Analysis^[2]

Cell Line:	PC3
Concentration:	0, 5, 10, 15, 20, 25 and 30 μM
Incubation Time:	0, 0.5, 1, 3, 6 and 9 h or 24 h (cell cycle)
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.

In Vivo

Clofoctol (175 mg/kg; i.p.; daily for 37 days) is capable of blocking tumour growth without apparent toxicity in a mouse model of human prostate cancer xenograft^[2].
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.

Animal Model:	Male athymic nude mice (BALB/c, nu/nu-NCr) aged 4–6 weeks, human prostate cancer xenograft model^[2]
Dosage:	175 mg/kg
Administration:	Intraperitoneal injection, daily for 37 days
Result:	Significantly inhibited PC3 tumour growth, tumour weight was also reduced by 60%.

Animal Model:	K18-hACE2 transgenic C57BL/6J mice with SARS-CoV-2 infection^[3]
Dosage:	62.5 mg/kg
Administration:	Intraperitoneal injection, 1h and 8h post-infection
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.

Animal Model:	8–10 week-old female C57BL/6J mice^[3]
Dosage:	62.5mg/kg
Administration:	Intraperitoneal injection, once (Pharmacokinetics)
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.

Molecular Weight

365.34

Formula

C₂₁H₂₆Cl₂O

CAS No.

37693-01-9

Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C(C(C)(C)CC(C)(C)C)C=C1CC2=CC=C(Cl)C=C2Cl

Structure Classification

Initial Source

Microorganisms

Bacillus subtilis

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (279 KB) SDS (0 KB)

COA (246 KB) HNMR (212 KB) RP-HPLC (115 KB)

Handling Instructions (2659 KB)

References

[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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Clofoctol37693-01-9BacterialSARS-CoVAntibioticSARS coronavirusprostate cancerSARS-CoV-2anticancerantibacterialantiviralInhibitorinhibitorinhibit

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