Terbinafine |
| Catalog No.GC17066 |
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.
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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.
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