| Size | Price | |
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| Other Sizes |
| Targets |
Climbazole targets the fungal enzyme cytochrome P450 14α-demethylase, which is involved in ergosterol biosynthesis. By inhibiting this enzyme, it disrupts the synthesis of ergosterol, a vital component of fungal cell membranes. This leads to increased membrane permeability and fungal cell death. It also induces rat hepatic cytochrome P450.
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| ln Vitro |
Aggressive prostate cancer (PCa) cells' exosome release is markedly inhibited by climbodium (20 µM; 48 hours) [1]. The protein concentrations of Rab27a and Alix are markedly inhibited by climbodium (20 µM), but not that of nSMase2[1]. Strongly inhibiting exosome formation and/or secretion is climbodium [2].
In vitro, Climbazole (20 μM; 48 hours) significantly decreases exosome secretion in aggressive prostate cancer (PCa) cells. It exhibits broad-spectrum activity against dermatophytes and yeast. It shows high in vitro efficacy against Pityrosporum ovale, which plays an important role in the pathogenesis of dandruff. |
| ln Vivo |
In vivo, Climbazole is effective in treating fungal skin infections such as dandruff and eczema. It has shown high in vivo efficacy against Pityrosporum ovale. It is used in cosmetic formulations and dermatological applications due to its efficacy and safety profile.
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| Enzyme Assay |
Climbazole is evaluated in cell-free enzymatic assays using purified cytochrome P450 14α-demethylase. The compound is incubated with the enzyme and a substrate, and the inhibition of enzyme activity is measured. IC50 values are determined to quantify the potency of inhibition.
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| Cell Assay |
Climbazole is assessed in cell-based assays using fungal cultures and mammalian cells. Its antifungal activity is tested against various fungal strains, and minimum inhibitory concentrations are determined. Its effects on exosome secretion are evaluated in prostate cancer cells.
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| Animal Protocol |
Climbazole is administered topically in animal models and in clinical settings to treat fungal infections. It is used in shampoos and creams for the treatment of dandruff and other fungal skin conditions. Efficacy is assessed by measuring fungal clearance and symptom improvement.
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| ADME/Pharmacokinetics |
Climbazole has a molecular weight of 292.76 and a molecular formula of C15H17ClN2O2. It has a CAS number of 38083-17-9. The compound is a solid. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Climbazole beyond its known use as a topical antifungal agent. It is generally considered safe for topical use. The compound is for research use and as a topical agent.
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| References | |
| Additional Infomation |
1-(4-Chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethylbut-2-one is a ketone in which 4-chlorophenoxy and 1H-imidazol-1-yl groups are substituted at the 1-position, and two methyl groups are substituted at the 3-position. It belongs to the monochlorobenzene class, imidazolium class, aromatic ether class, ketone class, and hemiacetal ether class.
Climbazole is also known as BAY-e 6975. It is a broad-spectrum imidazole antifungal agent with anti-dandruff properties. The compound is not approved for clinical use in all regions. |
| Molecular Formula |
C15H17CLN2O2
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|---|---|
| Molecular Weight |
292.76
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| Exact Mass |
292.097
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| CAS # |
38083-17-9
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| Related CAS # |
Climbazole-d4;1185117-79-6
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| PubChem CID |
37907
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
447.5±40.0 °C at 760 mmHg
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| Melting Point |
96-100°C
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| Flash Point |
224.4±27.3 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.561
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| LogP |
3.25
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
20
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| Complexity |
335
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OWEGWHBOCFMBLP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H17ClN2O2/c1-15(2,3)13(19)14(18-9-8-17-10-18)20-12-6-4-11(16)5-7-12/h4-10,14H,1-3H3
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| Chemical Name |
1-(4-chlorophenoxy)-1-imidazol-1-yl-3,3-dimethylbutan-2-one
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| Synonyms |
Climbazol; Baypival; Climbazole
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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 (~341.58 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.54 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 (8.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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 (8.54 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 | 3.4158 mL | 17.0788 mL | 34.1577 mL | |
| 5 mM | 0.6832 mL | 3.4158 mL | 6.8315 mL | |
| 10 mM | 0.3416 mL | 1.7079 mL | 3.4158 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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