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Climbazole Fungal inhibitor

Name: Climbazole
Brand: Selleck Chemicals
SKU: S4178
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4178

Climbazole(BAY-e 6975) is a broad-spectrum imidazole antifungal agent that can provide anti-dandruff benefits.

Chemical Structure

Molecular Weight: 292.76

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Quality Control

Batch: S417801 DMSO]59 mg/mL]false]Ethanol]59 mg/mL]false]Water]Insoluble]false Purity: 99.63%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.63

Related Targets	Integrase Bacterial Antibiotics Anti-infection Antiviral COVID-19 Parasite Reverse Transcriptase HIV HCV Protease
Other Fungal Inhibitors	Cycloheximide Tolnaftate Manogepix (E1210) Amorolfine HCl Thimerosal Isavuconazole Neticonazole Allicin Neticonazole Hydrochloride Juglone

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (201.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 59 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.950mg/ml (10.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 59 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.950mg/ml (10.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 59 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	292.76	Formula	C₁₅H₁₇ClN₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	38083-17-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BAY-e 6975			Smiles	CC(C)(C)C(=O)C(N1C=CN=C1)OC2=CC=C(C=C2)Cl

Mechanism of Action

In vitro	Climbazole has shown a high in vitro and in vivo efficacy against Pityrosporum ovale that appears to play an important role in the pathogenesis of dandruff. Its chemical structure and properties are similar to other fungicides such as ketoconazole and miconazole. For climbazole, the range of MICs is between < 0.06 and 1 μg/mL with an empirical median of 0.06 μg/mL.
In vivo	Climbazole is not mutagenic in the Salmonella typhimurium or Escherichia coli Ames assay and does not induce micronuclei in human lymphocytes. An in vivo mouse micronucleus test also shows it is non-mutagenic up to a maximum tolerated dose (MTD) of 150 mg/kg administered orally. In the in vivo/in vitro unscheduled DNA synthesis assay, climbazole shows no evidence of DNA damage in the livers of rats at doses up to the MTD of 200 mg/kg orally. A toxicokinetic study is performed in mice with oral administration of [¹⁴C]-climbazole (150 mg/kg). Radioactivity (20.42 μg-equiv./g plasma) is detected 15 min after oral administration of [¹⁴C]-climbazole, and the peak concentration is 62.96 μg-equiv./g plasma at 8 h after dosing.
References	[1] http://onlinelibrary.wiley.com/doi/10.1111/j.1439-0450.1997.tb00964.x/abstract [2] https://pubmed.ncbi.nlm.nih.gov/18950734/

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