Terbinafine HCl

Synonyms: KWD 201,KWD 2019,TDT 067 hydrochloride

Terbinafine HCl (KWD 201,KWD 2019,TDT 067 hydrochloride) inhibits ergosterol synthesis by inhibiting squalene epoxidase, used as an antifungal drug.

Terbinafine HCl  Chemical Structure

Terbinafine HCl Chemical Structure

CAS: 78628-80-5

Selleck's Terbinafine HCl has been cited by 4 publications

Purity & Quality Control

Batch: Purity: 100%
100

Choose Selective Fungal Inhibitors

Biological Activity

Description Terbinafine HCl (KWD 201,KWD 2019,TDT 067 hydrochloride) inhibits ergosterol synthesis by inhibiting squalene epoxidase, used as an antifungal drug.
Targets
squalene epoxidase [1]
In vitro
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]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05578950 Completed Onychomycosis Combined Military Hospital Abbottabad March 1 2022 Phase 1
NCT04880980 Completed Dermatophyte Infection|Terbinafine Adverse Reaction|Itraconazole Adverse Reaction Pak Emirates Military Hospital March 15 2021 Phase 3
NCT04188574 Completed Distal Subungual Onychomycosis|Fungal Infection|Fungus Nail Blueberry Therapeutics|IQVIA Biotech March 22 2021 Phase 2
NCT01484145 Completed Onychomycosis Nitric BioTherapeutics Inc December 2011 Phase 2
NCT01772212 Completed Mycoses GlaxoSmithKline February 24 2011 Phase 1

Chemical lnformation & Solubility

Molecular Weight 327.89 Formula

C21H25N.HCl

CAS No. 78628-80-5 SDF Download Terbinafine HCl SDF
Smiles CC(C)(C)C#CC=CCN(C)CC1=CC=CC2=CC=CC=C21.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 66 mg/mL ( (201.28 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 66 mg/mL

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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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