1. Anti-infection Autophagy
  2. Fungal Bacterial Autophagy Antibiotic
  3. Clotrimazole

Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity.

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

Clotrimazole Chemical Structure

Clotrimazole Chemical Structure

CAS No. : 23593-75-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
500 mg USD 55 In-stock
1 g USD 66 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Clotrimazole:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity.

IC50 & Target

Antifungal; CYP

Cellular Effect
Cell Line Type Value Description References
A549 IC50
5.1 μM
Compound: 1, CLT
Antiproliferative activity against human A549 cells by SRB assay
Antiproliferative activity against human A549 cells by SRB assay
[PMID: 19027297]
COS-7 IC50
0.07 μM
Compound: Clotrimazole
Inhibition of human cloned IK1 expressed in african green monkey COS7 cells by whole cell patch clamp assay
Inhibition of human cloned IK1 expressed in african green monkey COS7 cells by whole cell patch clamp assay
[PMID: 19282171]
CV-1 IC50
0.69 μM
Compound: 2
Inverse agonist activity at human CAR-LBD transfected in CV-1 cells after 24 hrs by luciferase reporter gene assay
Inverse agonist activity at human CAR-LBD transfected in CV-1 cells after 24 hrs by luciferase reporter gene assay
[PMID: 26717202]
HaCaT EC50
15 μM
Compound: Clotrimazole
Inhibition of human HaCaT cell proliferation after 48 hrs
Inhibition of human HaCaT cell proliferation after 48 hrs
[PMID: 19282171]
HEK293 IC50
0.59 μM
Compound: Clotrimazole
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
[PMID: 22761000]
HEK293 IC50
11.97 μM
Compound: Clotrimazole
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
[PMID: 28230985]
HEK-293T IC50
5.9 μM
Compound: Clotrimazole
Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
[PMID: 23122865]
HEK-293T IC50
51.6 μM
Compound: Clotrimazole
Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
[PMID: 23122865]
HEK-293T CC50
7 μg/mL
Compound: Clotrimazole
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 27720324]
HeLa IC50
1.4 μM
Compound: Clotrimazole
Inhibition of p97 in human HeLa cells assessed as reduction in p97-dependent UbG76V-GFP degradation incubated for 1 hr by luciferase reporter gene assay
Inhibition of p97 in human HeLa cells assessed as reduction in p97-dependent UbG76V-GFP degradation incubated for 1 hr by luciferase reporter gene assay
[PMID: 31550150]
HEp-2 CC50
18 μg/mL
Compound: Clotrimazole
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 24 hrs by trypan blue exclusion assay
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 24 hrs by trypan blue exclusion assay
[PMID: 27100030]
HEp-2 CC50
38 μg/mL
Compound: C
Cytotoxicity against human Hep2 cells assessed as reduction of cell viability after 24 hrs by trypan blue exclusion assay
Cytotoxicity against human Hep2 cells assessed as reduction of cell viability after 24 hrs by trypan blue exclusion assay
[PMID: 23702472]
HEp-2 CC50
38 μg/mL
Compound: Clotrimazole
Cytotoxicity against human Hep2 cells assessed as cell survival after 24 hrs by trypan blue exclusion method
Cytotoxicity against human Hep2 cells assessed as cell survival after 24 hrs by trypan blue exclusion method
[PMID: 26562544]
HEp-2 CC50
38.8 μg/mL
Compound: Clotrimazole
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability incubated for 24 hrs by trypan blue dye exclusion assay
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability incubated for 24 hrs by trypan blue dye exclusion assay
[PMID: 28963991]
HEp-2 EC50
40 μg/mL
Compound: C
Cytotoxicity against human Hep2 cells assessed as cell survival fraction after 24 hrs by trypan blue exclusion method
Cytotoxicity against human Hep2 cells assessed as cell survival fraction after 24 hrs by trypan blue exclusion method
[PMID: 22560629]
HEp-2 EC50
48 μg/mL
Compound: C
Antiproliferative activity against human Hep2 cells assessed as cell survival fraction after 24 hrs by MTT assay
Antiproliferative activity against human Hep2 cells assessed as cell survival fraction after 24 hrs by MTT assay
[PMID: 22560629]
LLC-PK1 IC50
3.5 μM
Compound: Clotrimazole
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
4.8 μM
Compound: Clotrimazole
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
6.7 μM
Compound: Clotrimazole
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
MCF7 CC50
5 μg/mL
Compound: Clotrimazole
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 27720324]
NIH3T3 IC50
289.45 μg/mL
Compound: Clotrimazole
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 29274492]
Ventricular myocyte IC50
20 μM
Compound: Clotrimazole
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
In Vitro

Clotrimazole (brand name Canesten or Lotrimin) is an antifungal medication commonly used in the treatment of fungal infections (of both humans and other animals) such as vaginal yeast infections, oral thrush, and ringworm. It is also used to treat athlete's foot and jock itch.It is commonly available as an over-the-counter substance in various dosage forms, such as a cream, and also (especially in the case of ear infection) as a combination medicine. It is also available as a troche or throat lozenge (prescription only). For ear infection, it is often applied in liquid form, as ear drops.? The antimycotic drug clotrimazole inhibits the function of the gastric H,K-ATPase in a manner similar to that observed for the Na,K-ATPase. Because of the high hydrophobicity of the compound, the interaction between clotrimazole and the ion pump occurs at the membrane domain in the apolar core of the membrane. The enzymatic activity was inhibited with a half-saturating concentration of 5.2 microM. Various partial reactions of the pump cycle were analyzed with the electrochromic styryl dye RH421 that has been widely used to study the transport mechanism of P-type ATPases.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

344.84

Formula

C22H17ClN2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=CC=C1C(N2C=CN=C2)(C3=CC=CC=C3)C4=CC=CC=C4

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 : 33.33 mg/mL (96.65 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 2.8999 mL 14.4995 mL 28.9990 mL
5 mM 0.5800 mL 2.8999 mL 5.7998 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (7.25 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 (7.25 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 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
References

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 2.8999 mL 14.4995 mL 28.9990 mL 72.4974 mL
5 mM 0.5800 mL 2.8999 mL 5.7998 mL 14.4995 mL
10 mM 0.2900 mL 1.4499 mL 2.8999 mL 7.2497 mL
15 mM 0.1933 mL 0.9666 mL 1.9333 mL 4.8332 mL
20 mM 0.1450 mL 0.7250 mL 1.4499 mL 3.6249 mL
25 mM 0.1160 mL 0.5800 mL 1.1600 mL 2.8999 mL
30 mM 0.0967 mL 0.4833 mL 0.9666 mL 2.4166 mL
40 mM 0.0725 mL 0.3625 mL 0.7250 mL 1.8124 mL
50 mM 0.0580 mL 0.2900 mL 0.5800 mL 1.4499 mL
60 mM 0.0483 mL 0.2417 mL 0.4833 mL 1.2083 mL
80 mM 0.0362 mL 0.1812 mL 0.3625 mL 0.9062 mL
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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.

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Clotrimazole
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