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Climbazole

Name: Climbazole
Brand: TargetMol
SKU: T1403
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1403Cas No. 38083-17-9

Alias BAY-e 6975

Climbazole (BAY-e 6975) is a broad-spectrum imidazole antifungal agent with anti-dandruff properties.

Climbazole

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Purity: 98.23%

Catalog No. T1403Alias BAY-e 6975Cas No. 38083-17-9

Climbazole (BAY-e 6975) is a broad-spectrum imidazole antifungal agent with anti-dandruff properties.

Pack Size	Price	USA Warehouse	Global Warehouse
1 g	$36	In Stock	In Stock
5 g	$87	-	In Stock
10 g	$127	-	In Stock
1 mL x 10 mM (in DMSO)	$30	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.23%

Appearance:Solid

Color:White

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COA LCMS HPLC HNMR

Product Introduction

Climbazole AI Summary

Climbazole exhibits a broad spectrum of bioactivity across various biological targets and assays, highlighting its potential for diverse therapeutic applications. It shows inhibitory effects against the Menin-MLL interaction in MLL-related leukemias, malarial parasite plastid, and the Ebola virus entry. Additionally, it demonstrates appreciable inhibition of human tyrosyl-DNA phosphodiesterase 1 (TDP1), gametocytocidal compounds, and Schwann cell intronic element firefly luciferase. In the context of retinoic acid metabolism, Climbazole functions as a RAMBA, showing potent CYP3A4 inhibition with an IC50 value of 100.0 nM. This activity was further confirmed in pig liver microsomal assays with an IC50 of 47500.0 nM. The compound also shows antiviral activity against SARS-CoV-2, demonstrating a reduction in cell viability in infected Vero E6 and Caco-2 cells, with inhibition levels of 22.58% at 10 µM and cytotoxicity inhibition percentages of 0.47% and 0.19% at the same concentration. Further analyses reveal that Climbazole inhibits transglutaminase in human keratinocytes with an IC50 of 4470.0 nM and exhibits significant cytochrome P450 inhibition in rat liver microsomes. It also showcases moderate inhibition against the SARS-CoV-2 3CL-Pro protease at 20µM, with inhibition percentages of 32.01% and 11.3%. Enzymatic assays indicate that Climbazole inhibits the human HDAC6 enzyme more effectively with a commercial peptide substrate (22.36%) as compared to a custom peptide (5.32%). Additionally, it binds with notable affinity to human SLC6A3, SLC6A2, SLC6A4, and ADORA3, while displaying antagonist activity at human CHRM1 and ADRA1A, and agonist activity at human CHRM1. Finally, it shows inhibition potential against human PTGS1 and ACHE, albeit with higher AC50 values. Overall, Climbazole's wide-ranging inhibitory activities and binding affinities, across multiple assays and biological targets, support its potential utility in therapeutic interventions against various diseases..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Climbazole (BAY-e 6975) is a broad-spectrum imidazole antifungal agent with anti-dandruff properties.
In vitro	The MICs of Climbazole ranged from <0.06 to 1 μg/mL, with a median value of 0.06 μg/mL. Climbazole showed high in vitro and in vivo efficacy against Pityrosporum ovale, which may be a major cause of dandruff.
In vivo	The MICs of Climbazole ranged from <0.06 to 1 μg/mL, with a median value of 0.06 μg/mL. Climbazole showed high in vitro and in vivo efficacy against Pityrosporum ovale, which may be a major cause of dandruff.
Synonyms	BAY-e 6975

Chemical Properties

Molecular Weight	292.76
Formula	C₁₅H₁₇ClN₂O₂
Cas No.	38083-17-9
Smiles	C(OC1=CC=C(Cl)C=C1)(C(C(C)(C)C)=O)N2C=CN=C2
Relative Density.	1.321 g/cm3. Temperature:20 °C.;1.317 g/cm3. Temperature:20 °C.

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 55 mg/mL (187.87 mM), Sonication is recommended.

DMSO: 50 mg/mL (170.79 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.83 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	3.4158 mL	17.0788 mL	34.1577 mL	170.7884 mL
5 mM	0.6832 mL	3.4158 mL	6.8315 mL	34.1577 mL
10 mM	0.3416 mL	1.7079 mL	3.4158 mL	17.0788 mL
20 mM	0.1708 mL	0.8539 mL	1.7079 mL	8.5394 mL
50 mM	0.0683 mL	0.3416 mL	0.6832 mL	3.4158 mL
100 mM	0.0342 mL	0.1708 mL	0.3416 mL	1.7079 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc