特比萘芬 T6702

Product Introduction
Bioactivity


英文名: Terbinafine

描述: Terbinafine (TDT 067) 是念珠菌属的角鲨烯环氧化酶有效的非竞争性抑制剂，Ki 值为 30 nM。它具有抗真菌感染活性。

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 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]。

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 58 mg/mL (199.01 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 16.67 mg/mL (57.19 mM)


关键字: Fungal | bacteria | Candida | Inhibitor | squalene epoxidase | Terbinafine | Bacterial | Antibiotic | antibacterial activity | inhibit | TDT067 | TDT-067 | infections

相关产品: Levofloxacin hydrate | Antibacterial compound 1 | Rifampicin | Vaborbactam | Nithiamide | Ornidazole | Clinafloxacin | Ciclopirox | Meropenem trihydrate | Tizoxanide

相关库: Drug Repurposing Compound Library | Drug-Fragment Library | Drug-induced Liver Injury (DILI) Compound Library | Human Metabolite Library | Inhibitor Library | Pediatric Drug Library | EMA Approved Drug Library | Anti-Bacterial Compound Library | Orally Active Compound Library | Anti-Infection Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途