Clotrimazole Antineoplastic and Immunosuppressive Antibiotics inhibitor

Cat.No.S1606

Clotrimazole (BAY b 5097, FB 5097) alters the permeability of the fungal cell wall by inhibiting the biosynthesis of ergosterol, used in the treatment of fungal infections.
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Quality Control

Batch: Purity: 99.97%
99.97

Solubility

In vitro
Batch:

Ethanol : 69 mg/mL

DMSO : 11 mg/mL (31.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
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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.
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Chemical Information, Storage & Stability

Molecular Weight 344.84 Formula

C22H17ClN2

Storage (From the date of receipt)
CAS No. 23593-75-1 Download SDF Storage of Stock Solutions

Synonyms BAY b 5097, FB 5097 SMILES C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CN=C4

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Mechanism of Action

In vitro
Clotrimazole causes a sustained depletion of intracellular Ca2+ stores, which results in activation of PKR, phosphorylation of eIF2alpha, and thereby in inhibition of protein synthesis at the level of translation initiation. This compound preferentially decreases the expression of the growth promoting proteins cyclin A, E and D1, resulting in inhibition of cyclin-dependent kinase activity and blockage of cell cycle in G1. It inhibits ADP-ribose-activated currents in HEK-293 cells expressing recombinant human TRPM2(hTRPM2). This chemical (3 mM to 30 mM) produces an essentially complete inhibition of theTRPM2-mediated current. It antagonizes ADP-ribose-activated whole-cell and single-channel currents in the rat insulinoma cell-line CRI-G1. This compound (2 mM) causes a sharp decline in parasitemia, complete inhibition of parasite replication, and destruction of parasites and host cells within a single intraerythrocytic asexual cycle (approximately 48 hours). It effectively and rapidly inhibits parasite growth in five different strains of P. falciparum, in vitro, irrespective of their Chloroquine sensitivity.
In vivo
Clotrimazole stimulates a subset of capsaicin-sensitive and mustard oil-sensitive trigeminal neurons, and evoked nocifensive behavior and thermal hypersensitivity with intraplantar injection in mice. This compound-induced pain behavior is suppressed by the TRPV1-antagonist BCTC [(N-(-4-tertiarybutylphenyl)-4-(3-cholorpyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide)] and absent in TRPV1-deficient mice. It inhibits the cold and menthol receptor TRPM8, and blocks menthol-induced responses in capsaicin- and mustard oil-insensitive trigeminal neurons.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/18199759/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-27)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06349122 NOT_YET_RECRUITING
Bacterial Vaginosis; Vaginal Dysbiosis; Premature Delivery
Assistance Publique Hopitaux De Marseille
2026-10 PHASE3
NCT07331792 NOT_YET_RECRUITING
Pityriasis Versicolor
Combined Military Hospital Abbottabad
2026-02-02 PHASE1; PHASE2
NCT07535424 COMPLETED
Otomycosis
Mayo Hospital Lahore
2024-11-20
NCT07441005 COMPLETED
Tinea Cruris
Hayat Abad Medical Complex, Peshawar
2025-05-15 EARLY_PHASE1
NCT06835361 RECRUITING
Candidal Vulvovaginitis (ICD-10 Code: B37.3); Vulvovaginal Candidiasis (VVC)
AVVA Pharmaceuticals Ltd.
2024-02-29 PHASE2; PHASE3
NCT07718685 COMPLETED
Dermatophytoses
Shalamar Institute of Health Sciences
2025-01-01

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