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Terbinafine

Terbinafine
Terbinafine (TDT 067) is a synthetic allylamine derivative with antifungal activity. Terbinafine exerts its effect through inhibition of squalene epoxidase, thereby blocking the biosynthesis of ergosterol, an important component of fungal cell membranes. As a result, this agent disrupts fungal cell membrane synthesis and inhibits fungal growth.
Catalog No. T6702Cas No. 91161-71-6
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Terbinafine

Catalog No. T6702Cas No. 91161-71-6
Terbinafine (TDT 067) is a synthetic allylamine derivative with antifungal activity. Terbinafine exerts its effect through inhibition of squalene epoxidase, thereby blocking the biosynthesis of ergosterol, an important component of fungal cell membranes. As a result, this agent disrupts fungal cell membrane synthesis and inhibits fungal growth.
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Pack SizePriceAvailabilityQuantity
50 mg$38In Stock
100 mg$46In Stock
200 mg$79In Stock
1 mL x 10 mM (in DMSO)$50In Stock
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Product Introduction

Bioactivity
Description
Terbinafine (TDT 067) is a synthetic allylamine derivative with antifungal activity. Terbinafine exerts its effect through inhibition of squalene epoxidase, thereby blocking the biosynthesis of ergosterol, an important component of fungal cell membranes. As a result, this agent disrupts fungal cell membrane synthesis and inhibits fungal growth.
Targets&IC50
SE:30 nM(Ki)
In vitro
Terbinafine (50 μM to 100 μM) inhibits only marginally the metabolism of ethoxycoumarin (CYP1A2), tolbutamide (CYP2C9), or ethynylestradiol, CsA, and cortisol. Terbinafine proves to be a potent inhibitor of the CYP2D6-mediated dextromethorphan O-demethylation and bufuralol 1-hydroxylation with IC50values of 0.2 μM and 0.25 μM, respectively. [1] Terbinafine is highly activ Aspergillus isolates (minimum inhibitory concentration [MIC] 0.01 to 2 mg/mL) with a primary fungicidal action (minimum fungicidal concentration [MFC] 0.02 to 4 mg/mL). [2] Terbinafine inhibits dextromethorphan O-demethylation with an apparent Ki ranging from 28 to 44 nM in human hepatic microsomes and averaging 22.4 nM for the heterologously expressed enzymes. [3] Terbinafine shows a very strong activity in vitro against Penicillium spp., Paecilomyces spp., Trichoderma spp., Acremonium spp. and Arthrographis spp. with GMs <1 mg/L. [4] Terbinafine decreases the levels of phosphorylated extracellular signal-regulated kinase (ERK). Terbinafine might cause a decrease of MEK, which in turn up-regulates p53 through the inhibition of ERK phosphorylation, and finally causes an increase of p21expression and cell-cycle arrest. [5]
In vivo
Terbinafine demonstrates efficacy not only when administered topically but also shows remarkable effectiveness in treating experimental dermatophytoses upon oral administration. In fungal-infected guinea pigs, there is a significant reduction in skin temperature following the fourth dose of terbinafine[6].
AliasTerbinex, SF 86-327, Lamisil, TDT 067
Chemical Properties
Molecular Weight291.43
FormulaC21H25N
Cas No.91161-71-6
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 58 mg/mL (199.01 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 16.67 mg/mL (57.19 mM)
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM3.4314 mL17.1568 mL34.3136 mL171.5678 mL
5 mM0.6863 mL3.4314 mL6.8627 mL34.3136 mL
10 mM0.3431 mL1.7157 mL3.4314 mL17.1568 mL
20 mM0.1716 mL0.8578 mL1.7157 mL8.5784 mL
50 mM0.0686 mL0.3431 mL0.6863 mL3.4314 mL
Ethanol
1mg5mg10mg50mg
100 mM0.0343 mL0.1716 mL0.3431 mL1.7157 mL

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