| 名称 | Terbinafine hydrochloride |
| 描述 | Terbinafine hydrochloride (KWD 2019) is a synthetic allylamine derivative structurally related to naftifine. Terbinafine is active against dermatophytes. |
| 体外活性 | Terbinafine (50 μM to 100 μM) inhibits only marginally the metabolism of ethoxycoumarin (CYP1A2), tolbutamide (CYP2C9), or ethynylestradiol, CsA, and cortisol. Terbinafine proves to be a potent inhibitor of the CYP2D6-mediated dextromethorphan O-demethylation and bufuralol 1-hydroxylation with IC50values of 0.2 μM and 0.25 μM, respectively. [1] Terbinafine is highly activ Aspergillus isolates (minimum inhibitory concentration [MIC] 0.01 to 2 mg/mL) with a primary fungicidal action (minimum fungicidal concentration [MFC] 0.02 to 4 mg/mL). [2] Terbinafine inhibits dextromethorphan O-demethylation with an apparent Ki ranging from 28 to 44 nM in human hepatic microsomes and averaging 22.4 nM for the heterologously expressed enzymes. [3] Terbinafine shows a very strong activity in vitro against Penicillium spp., Paecilomyces spp., Trichoderma spp., Acremonium spp. and Arthrographis spp. with GMs <1 mg/L. [4] Terbinafine decreases the levels of phosphorylated extracellular signal-regulated kinase (ERK). Terbinafine might cause a decrease of MEK, which in turn up-regulates p53 through the inhibition of ERK phosphorylation, and finally causes an increase of p21expression and cell-cycle arrest. [5] |
| 体内活性 | Terbinafine demonstrates efficacy both as a topical application and through oral administration in experimental dermatophytoses. Notably, in guinea pigs infected with fungi, a significant decrease in skin temperature is observed after the fourth terbinafine treatment[6]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (152.49 mM), Sonication is recommended.
|
| 关键字 | bacteria | Fungal | antibacterial activity | TDT-067 | infections | Bacterial | KWD-2019 | TDT 067 Hydrochloride | TDT-067 Hydrochloride | TDT067 Hydrochloride | Inhibitor | TDT067 | KWD2019 | Terbinafine hydrochloride | squalene epoxidase | Candida | Terbinafine Hydrochloride | Terbinafine | inhibit | Antibiotic | TDT 067 |
| 相关库 | 经典已知活性库 | EMA 上市药物库 | 天然产物库 | 药物功能重定位化合物库 | 抑制剂库 | 高通量筛选天然产物库 | FDA 上市药物库 | 抗感染天然产物库 | 已知活性化合物库 |
United States
