CAS |
91161-71-6 |
Chinese Name |
特比萘芬 |
English Name |
Terbinafine Hydrochloride |
Synonyms |
TDT 067;SF 86-327;Lamisil;Terbinex |
Molecular Formula |
C21H25N |
Molecular Weight |
291.43 |
Solubility |
Soluble in DMSO ≥25mg/mL |
Purity |
HPLC≥98% |
Appearance |
White to yellow Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC |
EINECS 245-385-8 |
MDL |
MFCD00242672 |
SMILES |
CN(C/C=C/C#CC(C)(C)C)CC1=C2C=CC=CC2=CC=C1 |
InChIKey |
DOMXUEMWDBAQBQ-WEVVVXLNSA-N |
InChI |
InChI=1S/C21H25N/c1-21(2,3)15-8-5-9-16-22(4)17-19-13-10-12-18-11-6-7-14-20(18)19/h5-7,9-14H,16-17H2,1-4H3/b9-5+ |
PubChem CID |
1549008 |
Target Point |
Fungal |
Passage |
Anti-infection |
Background |
It is an allylamine antifungal compound, which inhibits squalene cyclooxygenase in the process of ergosterol synthesis in fungal cells, and enables squalene to accumulate in cells and play a bactericidal role. |
Biological Activity |
Terbinafine (TDT 067) 是治疗真菌感染的抗真菌药物。它是来自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。[1-2] |
IC50 |
Ki: 30nM(squalene epoxidase)[1] |
In Vitro |
特比萘芬在体外对大多数真菌病原体具有主要的杀真菌作用,包括皮肤真菌,二形和丝状真菌。特比萘芬在角鲨烯环氧化作用下特异性地抑制真菌麦角甾醇的生物合成。处理过的真菌细胞迅速积累中间体角鲨烯并且缺乏麦角甾醇途径的最终产物[1]。 |
In Vivo |
特比萘芬不仅在局部施用后具有活性,而且在口服给药后对实验性皮肤癣菌非常有效。在真菌感染的豚鼠中,特比萘芬第四次治疗后皮肤温度急剧下降[2]。 |
Animal Experiment |
豚鼠:已经机械脱毛的豚鼠的背部(腰部)用含有106cfu的杜氏假丝酵母的0.1mL沙氏葡萄糖2%肉汤感染。接种后48小时开始治疗。将试验化合物(特比萘芬)悬浮于2%的tylose和吐温80中,连续9天每天一次通过胃管给药,或者溶解在聚乙二醇400和乙二醇的混合物中,并在身体的感染部位涂抹。用Hrigalski刮刀每天一次,连续1-7天,体积为0.4 mL [2]。 |
Data Literature Source |
[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]. Mieth H,et al. Preclinical evaluation of terbinafine in vivo. Clin Exp Dermatol. 1989 Mar;14(2):104-7. |
Unit |
Piece |
Specification |
100mg 10mM*1mL in DMSO 200mg 500mg |