| Description | Terbinafine (TDT 067) is a synthetic allylamine derivative with antifungal activity. Terbinafine exerts its effect through inhibition of squalene epoxidase, thereby blocking the biosynthesis of ergosterol, an important component of fungal cell membranes. As a result, this agent disrupts fungal cell membrane synthesis and inhibits fungal growth. |
| In vitro | Terbinafine（50 μM 至 100 μM）对乙氧基香豆素（CYP1A2）、托布他胺（CYP2C9）或乙炔雌醇、CsA 和皮质醇的代谢只有边缘性抑制作用。研究表明，Terbinafine是对CYP2D6介导的右美沙芬 O-去甲基化和布洛芬醇1-羟基化的强效抑制剂，其IC50值分别为0.2 μM 和 0.25 μM。[1] Terbinafine对曲霉属分离物具有高度活性（最小抑制浓度 [MIC] 0.01 至 2 mg/mL），其主要具有杀真菌作用（最小杀真菌浓度 [MFC] 0.02 至 4 mg/mL）。[2] Terbinafine抑制右美沙芬O去甲基化，在人肝微粒体中的表观Ki值介于28至44 nM之间，对异源表达的酶平均为22.4 nM。[3] Terbinafine对镰刀菌属、曲霉属、木霉属、金霉属和关节壳属表现出非常强的体外活性，其几何均数（GMs）<1 mg/L。[4] Terbinafine能降低磷酸化的细胞外信号调节激酶（ERK）水平。通过抑制ERK磷酸化，Terbinafine可能导致MEK减少，进而通过上调p53增加p21表达和细胞周期停滞。[5] |
| In vivo | Terbinafine 不仅在局部应用后具有活性，而且在口服给药后对实验性皮肤癣菌病具有极高的效果。在受真菌感染的豚鼠中，经过第四次 Terbinafine 治疗后，皮肤温度显著下降[6]。 |
| Target activity | SE:30 nM(Ki) |
| Synonyms | Terbinex, 特比萘芬, SF 86-327, Lamisil, TDT 067 |
| molecular weight | 291.43 |
| Molecular formula | C21H25N |
| CAS | 91161-71-6 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | Ethanol: 58 mg/mL (199.01 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 16.67 mg/mL (57.19 mM) |
| References | 1. Vickers AE, et al. Drug Metab Dispos, 1999, 27(9), 1029-1038. 2. Ryder NS, et al. Med Mycol, 2001, 39(1), 91-95. 3. Abdel-Rahman SM, et al. Drug Metab Dispos, 1999, 27(7), 770-775. 4. Garcia-Effron G, et al. J Antimicrob Chemother, 2004, 53(6), 1086-1089. 5. Ho PY, et al. Toxicol Appl Pharmacol, 2008, 229(1), 86-93. |
| Citations | 1. Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9 2. Ye Z, Ai X, Yang K, et al.Targeting Microglial Metabolic Rewiring Synergizes with Immune Checkpoint Blockade Therapy for Glioblastoma.Cancer Discovery.2023 3. Liu Y, Wang Z, Jin H, et al.Squalene-epoxidase-catalyzed 24 (S), 25-epoxycholesterol synthesis promotes trained-immunity-mediated antitumor activity.Cell Reports.2024, 43(4). |