Terbinafine-hydrochloride-TDT-067-hydrochloride-DataSheet-生命科學試劑-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作靶點: Fungal作通路: Anti-infection儲存式: 4C, sealed storage, away from moisture* In solvent : -80C, 6 months; -20C, 1 mont

2、h (sealedstorage, away from moisture)溶解性數(shù)據(jù)體外實驗 DMSO : 60 mg/mL (182.99 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗 請根據(jù)您的實驗動物

3、和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄的儲備液，再依次添加助溶?為保證實驗結果的可靠性，體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.62 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.62 mM); Cle

4、ar solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.62 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Terbinafine hydrochloride (TDT 067 hydrochloride)治療真 感染的抗真 藥物。它 來念珠 屬的鯊烯環(huán)氧化酶有效的競爭性抑制劑， Ki值為30 nM。IC50 & Target Ki: 30 nM (squalene epox

5、idase) 1體外研究 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.體內研究 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