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Terbinafine

Catalog No. T6702 CAS 91161-71-6

Synonyms: Terbinex, SF 86-327, Lamisil, TDT 067

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Terbinafine, CAS 91161-71-6

Pack Size	Availability	Price/USD
50 mg	In stock	$ 38.00
100 mg	In stock	$ 46.00
200 mg	In stock	$ 79.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 100%

Purity: 99.77%

Biological Description

Chemical Properties

Storage & Solubility Information

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].

Synonyms	Terbinex, SF 86-327, Lamisil, TDT 067
Molecular Weight	291.43
Formula	C21H25N
CAS No.	91161-71-6

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 58 mg/mL (199.01 mM)

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

DMSO: 58 mg/mL (199.01 mM)

References and Literature

1. Vickers AE, et al. Drug Metab Dispos, 1999, 27(9), 1029-1038. 2. Ryder NS, et al. Med Mycol, 2001, 39(1), 91-95. 3. Abdel-Rahman SM, et al. Drug Metab Dispos, 1999, 27(7), 770-775. 4. Garcia-Effron G, et al. J Antimicrob Chemother, 2004, 53(6), 1086-1089. 5. Ho PY, et al. Toxicol Appl Pharmacol, 2008, 229(1), 86-93.

Citations

1. Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9 2. Ye Z, Ai X, Yang K, et al.Targeting Microglial Metabolic Rewiring Synergizes with Immune Checkpoint Blockade Therapy for Glioblastoma.Cancer Discovery.2023 3. Liu Y, Wang Z, Jin H, et al.Squalene-epoxidase-catalyzed 24 (S), 25-epoxycholesterol synthesis promotes trained-immunity-mediated antitumor activity.Cell Reports.2024, 43(4).

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library EMA Approved Drug Library Pediatric Drug Library Human Metabolite Library Anti-Fungal Compound Library FDA-Approved Drug Library Anti-Infection Compound Library Orally Active Compound Library Approved Drug Library

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Keywords

Terbinafine 91161-71-6 Microbiology/Virology Antibiotic Antibacterial Antifungal Fungal Terbinex bacteria Candida Inhibitor squalene epoxidase Bacterial antibacterial activity SF 86-327 inhibit TDT067 TDT-067 infections Lamisil TDT 067 inhibitor

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