特比萘芬作用機制 - Medchemexpress - MCE中國

1、Product Data SheetTerbinafineCat. No.: HY-17395ACAS No.: 91161-71-6分式: CHN分量: 291.43作靶點: Fungal; Bacterial作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (343.14 mM)H2O : 0.1 mg/mL (insoluble)* means soluble, but saturation unknown.

2、SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 3.4314 mL 17.1568 mL 34.3136 mL5 mM 0.6863 mL 3.4314 mL 6.8627 mL10 mM 0.3431 mL 1.7157 mL 3.4314 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適

3、當?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.58 mM); Clear solution此案可獲得 2.5 mg/mL (8.58 mM，飽和度未知) 的澄清溶液。以 1

4、 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.58 mM); Suspended solution; Need ultrasonicPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (8.58 mM) 的均勻懸濁液，懸濁液可于服和腹腔注射。以 1

5、mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.58 mM); Clear solution; Need ultrasonic此案可獲得 2.5 mg/mL (8.58 mM) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物

6、活性 Terbinafine (TDT 067)治療真 感染的抗真 藥物。它 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。Terbinafine 還對某些蘭陽性和蘭陰性細菌具有抗菌活性。IC & Target Ki: 30 nM (squalene epoxidase)1體外研究 Terbinafine has a primary fungicidal action in vitro against most fungal pathogens, including dermatophytes, anddimorphic and filamentous fungi. Te

7、rbinafine specifically inhibits fungal ergosterol biosynthesis at the point ofsqualene epoxidation. The treated fungal cells rapidly accumulate tlic intermediate squalene and become deficient inthe end-product of the pathway, ergosterol1.體內(nèi)研究 Terbinafine is not only active after topical application

8、but is very effective in experimental dermatophytoses followingoral administration. In fungi infected guinea-pigs, the skin temperature dropps dramatically after the fourth treatmentof terbinafine2.PROTOCOLAnimal Guinea-pigs: The backs (lumbar regions) of guinea-pigs, which have been mechanically de

9、pilated, are infected withAdministration 2 0.1 mL Sabourauds dextrose 2% broth containing 106 c.f.u. of Truhophyton mentagrophytes. The treatmentscommence 48 h post-inoculation. The test compounds (Terbinafine) are suspended in 2% tylose and Tween 80 andadministered via a stomach tube once daily on

10、9 consecutive days, or dissolved in a mixture of polyethylene glycol400 and etbanol and spread on the infected part ot the body in a volume of 0.4 mL with a Hrigalski spatula oncedaily for 1-7 consecutive days2.MCE has not independently confirmed the accuracy of these methods. They are for reference

11、 only.REFERENCES1. 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):104-7.3. Ciftci E, et al. Mupirocin vs terbinafine in impetigo.Indian J Pediatr. 2002 Aug;69(8):679-82.McePdfHeightPage 2 of 3 www.MedChemECaution: Product has not been fully valid