Terbinafine (Synonyms: TDT 067)

Name: Terbinafine
Brand: MedChemExpress
SKU: HY-17395A
Rating: 5.0 (17 reviews)

Cat. No.: HY-17395A Purity: 99.96%: Data Sheet
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Terbinafine (TDT 067) is an orally active and potent antifungal agent. Terbinafine is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a K_i of 30 nM. Terbinafine also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria. Terbinafine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

CAS No. : 91161-71-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	Get quote
5 g	Get quote

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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Terbinafine:

17 Publications Citing Use of MCE Terbinafine

Cell Proliferation/Viability Assay

Cell Imaging/Staining

Flow Cytometry

Bio/Physico-chemical Assay

IHC

In Vivo Efficacy Study

: Terbinafine purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2021 Aug;41(8):726-746. [Abstract]; Cell viabilities of CRC cell lines treated with Terbinafine at 10, 25, 50 μmol/L were accessed by CCK8 assay. DMSO was used as control.

: Terbinafine purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2021 Aug;41(8):726-746. [Abstract]; Colony formation of CRC cell lines treated with Terbinafine at 50 μmol/L. DMSO was used as control.

: Terbinafine purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2021 Aug;41(8):726-746. [Abstract]; Cell cycle analysis (G0/G1, S, G2/M phase) of HT29 cells treated with terbinafine at 10, 25, 50 μmol/L. DMSO was used as control.

: Terbinafine purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2021 Aug;41(8):726-746. [Abstract]; Intracellular cholesterol levels of HT29 or RKO cells treated with Terbinafine at 10, 25, 50 μmol/L were accessed by cholesterol measurement. DMSO was used as control.

: Terbinafine purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2021 Aug;41(8):726-746. [Abstract]; IHC analysis of Ki67 in HT29 and RKO cells‐derived xenograft tumors and treated with terbinafine (oral, 50 mg/kg).

: Terbinafine purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2021 Aug;41(8):726-746. [Abstract]; Tumor growth curve of RKO cells treated with terbinafine (oral, 50 mg/kg) in nude mice.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Terbinafine (TDT 067) is an orally active and potent antifungal agent. Terbinafine is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a K_i of 30 nM. Terbinafine also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria^[1]^[2]^[3]. Terbinafine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target

Ki: 30 nM (squalene epoxidase)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
J774	IC₅₀	88 μM Compound: Tbf	Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay	[PMID: 19110434]
J774	IC₅₀	88 μM Compound: Terbinafine, Tbf	Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay	[PMID: 18547811]
MRC5	CC₅₀	63 μM Compound: TRB	Cytotoxicity against human MRC5 cells Cytotoxicity against human MRC5 cells	[PMID: 20805398]
THP-1	IC₅₀	329.3 μM Compound: Tbf, Terbinafine	Cytotoxicity against human THP1 cells after 48 hrs Cytotoxicity against human THP1 cells after 48 hrs	[PMID: 17960923]
THP-1	IC₅₀	329.3 μM Compound: Tbf, terbinafine	Cytotoxicity against human THP1 cells assessed as reduction of cell viability after 48 hrs Cytotoxicity against human THP1 cells assessed as reduction of cell viability after 48 hrs	[PMID: 17287123]
Vero	IC₅₀	30.9 μg/mL Compound: TRB	Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay	[PMID: 23831506]

In Vitro

Terbinafine has a primary fungicidal action in vitro against most fungal pathogens, including dermatophytes, and dimorphic and filamentous fungi. Terbinafine specifically inhibits fungal ergosterol biosynthesis at the point of squalene epoxidation. The treated fungal cells rapidly accumulate tlic intermediate squalene^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Terbinafine is not only active after topical application but is very effective in experimental dermatophytoses following oral administration. In fungi infected guinea-pigs, the skin temperature dropps dramatically after the fourth treatment of terbinafine^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

291.43

Formula

C₂₁H₂₅N

CAS No.

91161-71-6

Appearance

Solid

Color

White to yellow

SMILES

CN(C/C=C/C#CC(C)(C)C)CC1=C2C=CC=CC2=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (343.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4314 mL	17.1568 mL	34.3136 mL
5 mM	0.6863 mL	3.4314 mL	6.8627 mL
10 mM	0.3431 mL	1.7157 mL	3.4314 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (8.58 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (8.58 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (249 KB) HNMR (133 KB) RP-HPLC (225 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Ryder NS, et al. Terbinafine: mode of action and properties of the squalene epoxidase inhibition. Br J Dermatol. 1992 Feb;126 Suppl 39:2-7. [Content Brief]

[2]. Mieth H, et al. Preclinical evaluation of terbinafine in vivo. Clin Exp Dermatol. 1989 Mar;14(2):104-7. [Content Brief]

[3]. Ciftci E, et al. Mupirocin vs terbinafine in impetigo.Indian J Pediatr. 2002 Aug;69(8):679-82. [Content Brief]

Animal Administration
^[2]

Guinea-pigs: The backs (lumbar regions) of guinea-pigs, which have been mechanically depilated, are infected with 0.1 mL Sabouraud's dextrose 2% broth containing 10⁶ c.f.u. of Truhophyton mentagrophytes. The treatments commence 48 h post-inoculation. The test compounds (Terbinafine) are suspended in 2% tylose and Tween 80 and administered via a stomach tube once daily on 9 consecutive days, or dissolved in a mixture of polyethylene glycol 400 and etbanol and spread on the infected part ot the body in a volume of 0.4 mL with a Hrigalski spatula once daily for 1-7 consecutive days^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Ryder NS, et al. Terbinafine: mode of action and properties of the squalene epoxidase inhibition. Br J Dermatol. 1992 Feb;126 Suppl 39:2-7. [Content Brief]

[2]. Mieth H, et al. Preclinical evaluation of terbinafine in vivo. Clin Exp Dermatol. 1989 Mar;14(2):104-7. [Content Brief]

[3]. Ciftci E, et al. Mupirocin vs terbinafine in impetigo.Indian J Pediatr. 2002 Aug;69(8):679-82. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4314 mL	17.1568 mL	34.3136 mL	85.7839 mL
	5 mM	0.6863 mL	3.4314 mL	6.8627 mL	17.1568 mL
	10 mM	0.3431 mL	1.7157 mL	3.4314 mL	8.5784 mL
	15 mM	0.2288 mL	1.1438 mL	2.2876 mL	5.7189 mL
	20 mM	0.1716 mL	0.8578 mL	1.7157 mL	4.2892 mL
	25 mM	0.1373 mL	0.6863 mL	1.3725 mL	3.4314 mL
	30 mM	0.1144 mL	0.5719 mL	1.1438 mL	2.8595 mL
	40 mM	0.0858 mL	0.4289 mL	0.8578 mL	2.1446 mL
	50 mM	0.0686 mL	0.3431 mL	0.6863 mL	1.7157 mL
	60 mM	0.0572 mL	0.2859 mL	0.5719 mL	1.4297 mL
	80 mM	0.0429 mL	0.2145 mL	0.4289 mL	1.0723 mL
	100 mM	0.0343 mL	0.1716 mL	0.3431 mL	0.8578 mL

Terbinafine Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Terbinafine91161-71-6TDT 067TDT067TDT-067FungalBacterialAntibioticinfectionsbacteriaCandidasqualene epoxidaseantibacterial activityInhibitorinhibitorinhibit

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Terbinafine (Synonyms: TDT 067)

Customer Review

Other Forms of Terbinafine:

Terbinafine Related Antibodies

17 Publications Citing Use of MCE Terbinafine

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Antibiotic Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Terbinafine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Terbinafine Related Classifications

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