Catalog No.S1606 Synonyms: BAY b 5097, FB 5097
Molecular Weight(MW): 344.84
Clotrimazole 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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|Description||Clotrimazole alters the permeability of the fungal cell wall by inhibiting the biosynthesis of ergosterol, used in the treatment of fungal infections.|
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. Clotrimazole 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. Clotrimazole inhibits ADP-ribose-activated currents in HEK-293 cells expressing recombinant human TRPM2(hTRPM2). Clotrimazole (3 mM to 30 mM) produces an essentially complete inhibition of theTRPM2-mediated current. Clotrimazole antagonizes ADP-ribose-activated whole-cell and single-channel currents in the rat insulinoma cell-line CRI-G1.  Clotrimazole (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). Clotrimazole 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. Clotrimazole-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. Clotrimazole inhibits the cold and menthol receptor TRPM8, and blocks menthol-induced responses in capsaicin- and mustard oil-insensitive trigeminal neurons. |
|In vitro||Ethanol||69 mg/mL (200.09 mM)|
|DMSO||11 mg/mL (31.89 mM)|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||BAY b 5097, FB 5097|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02582177||Not yet recruiting||Tinea||Ache Laboratorios Farmaceuticos S.A.||August 2017||Phase 3|
|NCT02907307||Not yet recruiting||Vulvovaginal Candidiasis||Medinova AG||May 2017||Phase 3|
|NCT03005353||Not yet recruiting||Infection, Fungal||Assiut University||February 2017||Phase 2|Phase 3|
|NCT03024502||Not yet recruiting||Vulvovaginal Candidiasis||University of Sao Paulo||January 2017||Phase 1|Phase 2|
|NCT02860845||Recruiting||Candidiasis|Vaginosis, Bacterial||Laboratorios Ordesa|Clever Instruments S.L.||July 2016||Phase 4|
|NCT02847286||Active, not recruiting||HIV- Prevention||International Partnership for Microbicides, Inc.||September 2015||Phase 1|
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