Terbinafine |
| カタログ番号GC17066 |
テルビナフィン (TDT 067) は、経口で有効な強力な抗真菌剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 91161-71-6
Sample solution is provided at 25 µL, 10mM.
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Terbinafine (TDT 067) is a novel allylamine antifungal agent and a potent noncompetitive squalene cyclooxygenase inhibitor (Ki value is 30 nM) that selectively inhibits squalene cyclooxygenase, leading to a decrease in ergosterol, which interferes with membrane function and cell growth[1-2].
Terbinafine stimulates ROS production in HaCaT cells and induces a HaCaT Cytotoxic response with IC50 values of 12.5-25 μg/mL, and the Terbinafine group exhibited moderate cell rounding and cell shrinkage compared to untreated control and vector control[3]. Terbinafine (0, 30, 60 and 120 μM) concentration-dependently increased the activity of the p21 promoter in HUVEC and induced HUVEC cell cycle arrest by upregulating the p21 protein[4].
Terbinafine showed good antifungal activity against cutaneous fungal disease in guinea pigs caused by Trichophyton mentagrophytes or Microsporum canis[5]. After oral administration of Terbinafine at a dose of 30 mg/kg, the maximum plasma levels in cats, greyhounds and red-tailed eagles were 3.22, 4.01 and 1.2 μg/ml, respectively. The differences in the half-life of Terbinafine were not significant in cats (8.01 h), greyhounds (8.6 h), and horses (8.1 h), whereas it was significantly prolonged in the red-tailed eagles (17.5 h) and the African penguins ( 17.0 h) were significantly prolonged[2].
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.
[2]. Wang A, Ding H, Liu Y, et al. Single dose pharmacokinetics of terbinafine in cats[J]. Journal of feline medicine and surgery, 2012, 14(8): 540-544.
[3]. Lam P L, Wong M M, Hung L K, et al. Miconazole and terbinafine induced reactive oxygen species accumulation and topical toxicity in human keratinocytes[J]. Drug and Chemical Toxicology, 2022, 45(2): 834-838.
[4]. Ho PY, Hsu SP, Liang YC, Kuo ML, Ho YS, Lee WS. Inhibition of the ERK phosphorylation plays a role in terbinafine-induced p21 up-regulation and DNA synthesis inhibition in human vascular endothelial cells. Toxicol Appl Pharmacol. 2008 May 15;229(1):86-93.
[5]. Petranyi G, Meingassner JG, Mieth H. Activity of terbinafine in experimental fungal infections of laboratory animals. Antimicrob Agents Chemother. 1987 Oct;31(10):1558-61.
| Cell experiment [1]: | |
Cell lines | HaCaT cells |
Preparation Method | Terbinafine was incubated with HaCaT cells for 24 hours, and DMSO (1%) and doxorubicin were used as control and positive control, respectively. Sulforhodamine B protein (SRB) staining was used to evaluate the cytotoxicity of Terbinafine on HaCaT cells. |
Reaction Conditions | 50、25、12.5、6.25、3.125 and 1.56 μg/mL, 24 h |
Applications | The IC50 value of Terbinafine against HaCaT cells was 12.5-25 μg/mL. IC50 values of Terbinafine showed moderate degree of cell rounding and cell shrinkage compared with untreated and vehicle controls. |
| Animal experiment [2]: | |
Animal models | Guinea Pig Model of Skin Infection |
Preparation Method | For treatment, Terbinafine is suspended in 2% methylcellulose and 0.5% Tween 80. Treatment began on the day of inoculation with Trichophyton mentagrophytes and continued once daily for 9 consecutive days. Mycologic status was assessed 24 hours after the last treatment. |
Dosage form | 2, 4, 6 and 8 mg/kg/day, oral, 9 days |
Applications | Oral dose of 4 to 6 mg/kg per day from the day of infection for good activity against Trichophytsis for 9 consecutive days. |
References: | |
| Cas No. | 91161-71-6 | SDF | |
| Chemical Name | (E)-N,6,6-trimethyl-N-(naphthalen-1-ylmethyl)hept-2-en-4-yn-1-amine | ||
| Canonical SMILES | CC(C)(C)C#CC=CCN(C)CC1=CC=CC2=CC=CC=C21 | ||
| Formula | C21H25N | M.Wt | 291.43 |
| 溶解度 | ≥ 11.9mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.)
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
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