Terbinafine-hydrochloride-TDT-067-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETerbinafine hydrochlorideCat. No.: HY-17395CAS No.: 78628-80-5Synonyms: TDT 067 hydrochloride分式: CHClN分量: 327.89作靶点: Fungal作通路: Anti-infection储存式: 4C, sealed storage, away from moisture* In solvent : -80C, 6 months; -20C, 1 mont

2、h (sealedstorage, away from moisture)溶解性数据体外实验 DMSO : 60 mg/mL (182.99 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.0498 mL 15.2490 mL 30.4980 mL5 mM 0.6100 mL 3.0498 mL 6.0996 mL10 mM 0.3050 mL 1.5249 mL 3.0498 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物

3、和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.62 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.62 mM); Cle

4、ar solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.62 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Terbinafine hydrochloride (TDT 067 hydrochloride)治疗真 感染的抗真 药物。它 来念珠 属的鲨烯环氧化酶有效的竞争性抑制剂， Ki值为30 nM。IC50 & Target Ki: 30 nM (squalene epox

5、idase) 1体外研究 Terbinafine has a primary fungicidal action in vitro against most fungal pathogens, including dermatophytes,and dimorphic and filamentous fungi. Terbinafine specifically inhibits fungal ergosterol biosynthesis at thepoint of squalene epoxidation. The treated fungal cells rapidly accumul

6、ate tlic intermediate squalene andbecome deficient in the end-product of the pathway, ergosterol 1.体内研究 Terbinafine is not only active after topical application but is very effective in experimental dermatophytosesfollowing oral administration. In fungi infected guinea-pigs, the skin temperature dro

7、pps dramatically after thefourth treatment of terbinafine 2.PROTOCOLAnimal Guinea-pigs: The backs (lumbar regions) of guinea-pigs, which have been mechanically depilated, areAdministration 2 infected with 0.1 mL Sabourauds dextrose 2% broth containing 106 c.f.u. of Truhophyton mentagrophytes.The tre

8、atments commence 48 h post-inoculation. The test compounds (Terbinafine) are suspended in 2%tylose and Tween 80 and administered via a stomach tube once daily on 9 consecutive days, or dissolved ina mixture of polyethylene glycol 400 and etbanol and spread on the infected part ot the body in a volum

9、e of0.4 mL with a Hrigalski spatula once daily for 1-7 consecutive days 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ryder NS, et al. Terbinafine: mode of action and properties of the squalene epoxidase inhibition. Br J Dermatol. 1992 Feb;126 Suppl39:2-8.2. Mieth H, et al. Preclinical evaluation of terbinafine in vivo. Clin Exp Dermatol. 1989 Mar;14(2):104-8.McePdfHeightCaution: Product has not been fully validated for