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MedKoo Cat#: 524755 | Name: Climbazole
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Climbazole is an imidazole-based antifungal agent primarily used in topical formulations to treat dandruff and seborrheic dermatitis. It works by inhibiting ergosterol synthesis in fungal cell membranes, disrupting membrane integrity and leading to fungal cell death. Climbazole is particularly effective against Malassezia species, a yeast implicated in scalp and skin conditions.

Chemical Structure

Climbazole
Climbazole
CAS#38083-17-9

Theoretical Analysis

MedKoo Cat#: 524755

Name: Climbazole

CAS#: 38083-17-9

Chemical Formula: C15H17ClN2O2

Exact Mass: 292.0979

Molecular Weight: 292.76

Elemental Analysis: C, 61.54; H, 5.85; Cl, 12.11; N, 9.57; O, 10.93

Price and Availability

Size Price Availability Quantity
5g USD 150.00 Ready to ship
10g USD 225.00 Ready to ship
20g USD 350.00 2 weeks
50g USD 550.00 2 weeks
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Synonym
Climbazole; Baypival; Climbazol; Baysan.
IUPAC/Chemical Name
1-(4-Chlorophenoxy)-1-(1H-imidazolyl)-3,3-dimethyl-2-butanone
InChi Key
YFPFGHKWUKVEFZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H17ClN2O2/c1-15(2,3)13(19)12(14-17-8-9-18-14)20-11-6-4-10(16)5-7-11/h4-9,12H,1-3H3,(H,17,18)
SMILES Code
CC(C)(C)C(C(OC1=CC=C(Cl)C=C1)C2=NC=CN2)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Certificate of Analysis
View CoA: current batch, Lot#C22B04B29
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
Biological target:
Climbazole (BAY-e 6975) is a potent antifungal agent that can provide anti-dandruff benefits and is also a potent inducer of rat hepatic cytochrome P450 as well as ergosterol synthesis.
In vitro activity:
After 24 h treatment with climbazole in the absence of S9-mix to concentrations ranging from 5 to 20 μg/mL, cytotoxicity, i.e., reduction in total cell growth, ranged from 0 to 93%. An increase of greater than 90 mutants per 106 clonable cells was observed at 15 μg/mL (mean induced mutant frequency 140) and 17.5 μg/mL (mean induced mutant frequency 135), with a no observable effect level (NOEL) of approximately 10 μg/mL. The data obtained on colony size distributions revealed an increase in the frequency of small colonies when the treated cultures were compared to the solvent control cultures. Such an effect may indicate damage to multiple loci on chromosome 11 in addition to functional loss of the tk locus. Under the conditions of the study, climbazole did not induce mutations in the mouse lymphoma assay in the absence and presence of metabolic activation after a 4 h treatment period. However, after an extended treatment period of 24 h in the absence of S9-mix, an increase mutant frequency was obtained indicative of a clastogenic or aneugenic effect. Reference: Mutat Res. 2009 Jan;672(1):27-39. https://pubmed.ncbi.nlm.nih.gov/18950734/
In vivo activity:
Based on the results of the dose-range finding studies, 150 mg/kg bw was determined to be the MTD. In the mouse bone marrow micronucleus test after oral administration of climbazole, all treatment and vehicle control groups exhibited normal frequencies of micronucleated polychromatic erythrocytes, while the positive control (CPA) induced a significant increase in MNPCE frequency demonstrating the sensitivity and responsiveness the test system. It can be concluded that climbazole did not induce micronuclei in mouse bone marrow after the administration of oral doses up to the MTD (150 mg/kg). However, there was no significant reduction in the ratio of PCEs to total erythrocytes, which is indicative of cytotoxicity and hence target tissue, i.e., bone marrow, exposure. Consequently a bioavailability study was carried out using [14C]-climbazole to support the in vivo micronucleus test by demonstrating the systemic bioavailability of climbazole after oral administration to mice. Reference: Mutat Res. 2009 Jan;672(1):27-39. https://pubmed.ncbi.nlm.nih.gov/18950734/
Solvent mg/mL mM comments
Solubility
DMSO 53.0 181.04
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 292.76 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Pérez-Rivera AA, Hu T, Aardema MJ, Nash JF. Evaluation of the genotoxicity of the imidazole antifungal climbazole: comparison to published results for other azole compounds. Mutat Res. 2009 Jan;672(1):27-39. doi: 10.1016/j.mrgentox.2008.09.011. Epub 2008 Oct 2. PMID: 18950734. 2. Kobayashi Y, Suzuki M, Ohshiro N, Sunagawa T, Sasaki T, Tokuyama S, Yamamoto T, Yoshida T. Climbazole is a new potent inducer of rat hepatic cytochrome P450. J Toxicol Sci. 2001 Aug;26(3):141-50. doi: 10.2131/jts.26.141. PMID: 11552297.
In vitro protocol:
1. Pérez-Rivera AA, Hu T, Aardema MJ, Nash JF. Evaluation of the genotoxicity of the imidazole antifungal climbazole: comparison to published results for other azole compounds. Mutat Res. 2009 Jan;672(1):27-39. doi: 10.1016/j.mrgentox.2008.09.011. Epub 2008 Oct 2. PMID: 18950734. 2. Kobayashi Y, Suzuki M, Ohshiro N, Sunagawa T, Sasaki T, Tokuyama S, Yamamoto T, Yoshida T. Climbazole is a new potent inducer of rat hepatic cytochrome P450. J Toxicol Sci. 2001 Aug;26(3):141-50. doi: 10.2131/jts.26.141. PMID: 11552297.
In vivo protocol:
1. Pérez-Rivera AA, Hu T, Aardema MJ, Nash JF. Evaluation of the genotoxicity of the imidazole antifungal climbazole: comparison to published results for other azole compounds. Mutat Res. 2009 Jan;672(1):27-39. doi: 10.1016/j.mrgentox.2008.09.011. Epub 2008 Oct 2. PMID: 18950734.
1: Yan J, Chen H, Ji Z, Tang Y, Wang S, Zheng J, Li H, Li L, Ge RS, Dong Y. Azole fungicides: Potential endocrine disrupting effects and impact on placental steroidogenesis via inhibiting human and rat 3β-hydroxysteroid dehydrogenase. Ecotoxicol Environ Saf. 2025 Jun 4;300:118471. doi: 10.1016/j.ecoenv.2025.118471. Epub ahead of print. PMID: 40472693. 2: So B, Park JH, Kim M, Lee H, Yoon JH, Lee YJ, Kim D, Kwon HW, Park J, Han T, Lee YH, Park JT. Rapid and Accurate Genotoxicity Assessment Using the Neutral Comet Assay in Cyprinus carpio Cells. Life (Basel). 2025 Apr 4;15(4):603. doi: 10.3390/life15040603. PMID: 40283158; PMCID: PMC12028690. 3: Jia W, Deng Y, Liu H, Yang J, Cao Q, Huang K, Li Y, Shi L, Ma Y. Nontargeted screening of contaminants of emerging concern in the Nandu River Estuary. Mar Pollut Bull. 2025 Jun;215:117870. doi: 10.1016/j.marpolbul.2025.117870. Epub 2025 Mar 26. PMID: 40147050. 4: Annunzi E, Luongo FP, Girolamo F, Ponchia R, Passaponti S, Piomboni P, Luddi A. In Vitro Exposure to the Endocrine-Disrupting Chemical Climbazole Impairs Human Sperm Motility, Hormonal Signalling, and Mitochondrial Activity. Cells. 2025 Mar 13;14(6):427. doi: 10.3390/cells14060427. PMID: 40136676; PMCID: PMC11940937. 5: Płatkiewicz J, Frankowski R, Cieślak A, Grześkowiak T, Zgoła-Grześkowiak A. Long-term study of azoles in surface water and treated wastewater. J Environ Manage. 2025 Apr;380:124820. doi: 10.1016/j.jenvman.2025.124820. Epub 2025 Mar 13. PMID: 40086272. 6: Schönrath I, Schmidtkunz C, Küpper K, Weber T, Leng G, Kolossa-Gehring M. Exposure of young German adults to the anti-dandruff agent climbazole from 2002 to 2022: Analysis of specific biomarkers in urinary samples. Chemosphere. 2024 Nov;367:143611. doi: 10.1016/j.chemosphere.2024.143611. Epub 2024 Oct 22. PMID: 39447771. 7: Yuan D, Zhang B. Assessing the chronic toxicity of climbazole to Daphnia magna: Physiological, biochemical, molecular, and reproductive perspectives. Comp Biochem Physiol C Toxicol Pharmacol. 2025 Jan;287:110061. doi: 10.1016/j.cbpc.2024.110061. Epub 2024 Oct 20. PMID: 39437869. 8: Sun C, Huang Y, Bakhtiari AR, Yuan D, Zhou Y, Zhao H. Long-term exposure to climbazole may affect the health of stress-tolerant coral Galaxea fascicularis. Mar Environ Res. 2024 Oct;201:106679. doi: 10.1016/j.marenvres.2024.106679. Epub 2024 Aug 10. PMID: 39153271. 9: Song W, Wang N, Li A, Ji X, Huang X, Wang T, Hao H. Multi-component Crystal Strategy for Improving Water Solubility and Antifungal Activity of Climbazole. Pharm Res. 2024 Aug;41(8):1737-1754. doi: 10.1007/s11095-024-03748-5. Epub 2024 Jul 29. PMID: 39078577. 10: Schönrath I, Schmidtkunz C, Ebert KE, Küpper K, Brüning T, Koch HM, Leng G. Human urinary excretion kinetics of the antimycotic climbazole: Biomonitoring of two new metabolites after oral and dermal dosage. Toxicol Lett. 2024 Aug;399:25-33. doi: 10.1016/j.toxlet.2024.06.011. Epub 2024 Jun 26. PMID: 38936562. 11: Ndiaye D, Perceau M, Lorcin M, Denis F, Gaté L. Antifungal climbazole alters androgenic pathways in mammalian cells. Toxicol In Vitro. 2024 Aug;99:105854. doi: 10.1016/j.tiv.2024.105854. Epub 2024 May 23. PMID: 38795739. 12: Ergin Ç, Kurt Ö, Türkoğlu M, Sevinç H, Akbaba G. Evaluation of novel cosmetic shampoo formulations against Malassezia species: Preliminary results of anti-dandruff shampoo formulations. J Cosmet Dermatol. 2024 Jun;23(6):2078-2083. doi: 10.1111/jocd.16219. Epub 2024 Mar 27. PMID: 38544350. 13: Lu ZJ, Shi WJ, Ma DD, Zhang JG, Long XB, Li SY, Gao FZ, Zhang QQ, Ying GG. The azole biocide climbazole induces oxidative stress, inflammation, and apoptosis in fish gut. Sci Total Environ. 2024 May 1;923:171475. doi: 10.1016/j.scitotenv.2024.171475. Epub 2024 Mar 6. PMID: 38453063. 14: Ipinmoroti AO, Pandit R, Crenshaw BJ, Sims B, Matthews QL. Human adenovirus type 3 restores pharmacologically inhibited exosomal cargo in lung carcinoma cells. Front Pharmacol. 2024 Feb 21;15:1339862. doi: 10.3389/fphar.2024.1339862. PMID: 38449802; PMCID: PMC10915030. 15: Iancu VI, Chiriac LF, Paun I, Pirvu F, Dinu C, Kim L, Pascu LF, Niculescu M. Occurrence and distribution of azole antifungal agents in eight urban Romanian waste water treatment plants. Sci Total Environ. 2024 Apr 10;920:170898. doi: 10.1016/j.scitotenv.2024.170898. Epub 2024 Feb 16. PMID: 38369155. 16: Paz-Alvarez M, Fung Tang C, Pudney PD, Lane ME. Rational development of topical climbazole formulations. Int J Pharm. 2024 Mar 25;653:123886. doi: 10.1016/j.ijpharm.2024.123886. Epub 2024 Feb 7. PMID: 38331330. 17: Lu ZJ, Shi WJ, Gao FZ, Ma DD, Zhang JG, Li SY, Long XB, Zhang QQ, Ying GG. An azole fungicide climbazole damages the gut-brain axis in the grass carp. J Hazard Mater. 2024 Mar 5;465:133463. doi: 10.1016/j.jhazmat.2024.133463. Epub 2024 Jan 10. PMID: 38219582. 18: Lu ZJ, Shi WJ, Gao FZ, Ma DD, Zhang JG, Li SY, Long XB, Zhang QQ, Ying GG. Climbazole causes cell apoptosis and lipidosis in the liver of grass carp. Aquat Toxicol. 2023 Oct;263:106698. doi: 10.1016/j.aquatox.2023.106698. Epub 2023 Sep 15. PMID: 37722153. 19: Denora M, Candido V, Brunetti G, De Mastro F, Murgolo S, De Ceglie C, Salerno C, Gatta G, Giuliani MM, Mehmeti A, Bartholomeus RP, Perniola M. Uptake and accumulation of emerging contaminants in processing tomato irrigated with tertiary treated wastewater effluent: a pilot-scale study. Front Plant Sci. 2023 Aug 23;14:1238163. doi: 10.3389/fpls.2023.1238163. PMID: 37692419; PMCID: PMC10484752. 20: Wang Y, Yin N, Yang R, Zhao M, Li S, Zhang S, Zhao Y, Faiola F. Development of a simplified human embryonic stem cell-based retinal pre-organoid model for toxicity evaluations of common pollutants. Cutan Ocul Toxicol. 2023 Dec;42(4):264-272. doi: 10.1080/15569527.2023.2249988. Epub 2023 Aug 27. PMID: 37602871.