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Terbinafine HCl Fungal inhibitor

Name: Terbinafine HCl
SKU: S2557
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S2557

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

Chemical Structure

Molecular Weight: 327.89

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.93%

99.93

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Chemical Information, Storage & Stability

Molecular Weight	327.89	Formula	C₂₁H₂₅N.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	78628-80-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	KWD 201,KWD 2019,TDT 067 hydrochloride			Smiles	CC(C)(C)C#CC=CCN(C)CC1=CC=CC2=CC=CC=C21.Cl

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (198.23 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 65 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	squalene epoxidase ^[1]
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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/10460803/ [2] https://pubmed.ncbi.nlm.nih.gov/11270414/ [3] https://pubmed.ncbi.nlm.nih.gov/10383919/ [4] https://pubmed.ncbi.nlm.nih.gov/15102749/ [5] https://pubmed.ncbi.nlm.nih.gov/18272192/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06295328	Recruiting	Chronic Hepatitis b	Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)	April 13 2022	Phase 1\|Phase 2
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

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