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 Ki 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.
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Terbinafine Estructura química
No. CAS :
91161-71-6
This product is a controlled substance and not for sale in your territory.
Based on 10 publication(s) in Google Scholar
Other Forms of Terbinafine:
Terbinafine hydrochloride
In-stock
Terbinafine-d7
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Terbinafine-d3 hydrochloride
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Terbinafine-d5 hydrochloride
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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 Ki 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]
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.
Terbinafine Related Antibodies
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.
Ensayo clínico
Peso molecular
291.43
Fòrmula
C21H25N
No. CAS
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
Envío
Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
2 years
-20°C
1 year
Solvente y solubilidad
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
ConcentrationSolventMass
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.
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.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO 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 μLDMSO 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 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
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.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
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.
[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]
Administraciòn de animales
[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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias
[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]
[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.
[2]. Mieth H, et al. Preclinical evaluation of terbinafine in vivo. Clin Exp Dermatol. 1989 Mar;14(2):104-7.
[3]. Ciftci E, et al. Mupirocin vs terbinafine in impetigo.Indian J Pediatr. 2002 Aug;69(8):679-82.
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.
Optional Solvent
ConcentrationSolventMass
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
Anti-infection
FungalBacterialAntibiotic
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.
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