米卡芬凈鈉作用機制 - Medchemexpress - MCE中國

1、Product Data SheetMicafungin sodiumCat. No.: HY-16321CAS No.: 208538-73-2分式: CHNNaOS分量: 1292.26作靶點: Fungal作通路: Anti-infection儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數據體外實驗 DMSO : 32 mg/mL (24.76 mM)* means soluble, but saturation unknown.Solvent

2、Mass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 0.7738 mL 3.8692 mL 7.7384 mL5 mM 0.1548 mL 0.7738 mL 1.5477 mL10 mM 0.0774 mL 0.3869 mL 0.7738 mL請根據產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品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。體內實驗請根據您

3、的實驗動物和給藥式選擇適當的溶解案。以下溶解案都請先按照 In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據儲存條件，適當保存；體內實驗的作液，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 (1.93 mM); Clear solution此案可獲得 2.5 mg/mL (1.93 mM，飽和度未

4、知) 的澄清溶液。以 1 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 (1.93 mM); Clear solution此案可獲得 2.5 mg/mL (1.93 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到

5、 900 L 20% 的 SBE-CD 理鹽溶液中，混合Page 1 of 2 www.MedChemE均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (1.93 mM); Clear solution此案可獲得 2.5 mg/mL (1.93 mM，飽和度未知) 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物活性 Micafungin sodium (FK 46

6、3 sodium)是抗真菌劑，抑制1, 3-beta-D-glucan的合成。體外研究 Micafungin (10 mg/mL) phenotypicly decreases the formation of biofilm in most of the isolates. For all the genestested, the levels of mRNA transcription are also decreased significantly in micafungin-treated samples cf. theiruntreated counterparts1. The co

7、mbination of micafungin and KB425796-C is fungicidal and markedly reduces thenumber of CFU, in contrast to the fungistatic effects (no reduction in CFU) observed at all examined time points wheneach drug is used alone2.體內研究 Micafungin (1 mg/kg) significantly prolongs survival compared with mice admi

8、nistered saline. Animals given acombination of micafungin (0.1 mg/kg) and KB425796-C (32 mg/kg) show a trend towards prolonged survival in comparison with those treated with micafungin (0.1 mg/kg) alone. In the livers of micafungin-treated mice, thenumber of CFUs decreases, although the clearance ef

9、fect is less than that found in the kidneys. Combinationtreatment with micafungin and KB425796-C results in a significant decrease in the number of CFUs compared withthe treatment with micafungin alone at all examined doses. The clearance effect associated with KB425796-C incombination with micafung

10、in is greater than that observed in AMPH-treated animals2.PROTOCOLCell Assay 2 Each fungal isolate is incubated statically in yeast-maltose (YM) agar broth for 24 h at 30C. Cryptococcusneoformans YC203 is grown in YM broth medium for 20 h at 30C with shaking at 200 r.p.m. A cell suspension isprepare

11、d by washing the cultured cells once with sterile saline. A. fumigatus FP1305 is cultured on a potato dextroseagar (PDA) slant for 4 days, and spores are then harvested in sterile saline and collected by filtering through gauze.Antifungal activity against all isolates, with the exception of C. neofo

12、rmans, is measured by the micro-broth dilutionmethod in 96-well culture plates using RPMI 1640 medium supplemented with l-glutamine, but without sodiumbicarbonate, and buffered to pH 7.0 with 0.165 m MOPS. ForC. neoformans, yeast nitrogen base-glucose (YNBD)medium is used. For the assay, the test mi

13、croorganism is inoculated into each well to yield 1105 CFU/well, and theplates are then incubated for 20 h or 48 h at 37C. Two end points are determined by microscopic observation: MEC,which is defined as a substantial reduction in fungal growth, and MIC, which is defined as a complete inhibition of

14、growth.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Eight groups of ten female DBA/2 mice (7 weeks old) are intravenously injected with 2.0106 A. fumigatus FP1305Administration 2 spores. The test groups receive the following treatments: AMPH a

15、t 1 mg/kg of body weight/dose givenintraperitoneally (i.p.) once daily (q.d.); micafungin at 0.1, 0.32 or 1 mg/kg of body weight/dose given subcutaneously(s.c.) (q.d.); micafungin given s.c. (0.1, 0.32 or 1 mg/kgq.d.) plus KB425796-C given i.p. (32 mg/kg) twice daily (b.i.d.);and saline (b.i.d.). Dr

16、ugs are administered on days 1 and 2. Five mice in each group are killed 1 day after thecompletion of treatment. The livers and kidneys are aseptically removed, and each organ is then homogenized in 5mL sterile saline. Serial 10-fold dilutions of the homogenates are plated on PDA and incubated for 4

17、8 h at 37C, andthe numbers of CFU per gram of tissue are then calculated. The survival rate of remaining five mice of each group arePage 2 of 3 www.MedChemEexamined daily for 31 days after the challenge.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使

18、本產品發(fā)表的科研獻 J Antimicrob Chemother. 2020 May 9. pii: dkaa157. J Clin Microbiol. 2017 Jun;55(6):1883-1893. PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. mSphere. 2018 Nov 14;3(6). pii: e00547-18. Sci Rep. 2017 Feb 17;7:42886.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Bazzi W, et al. The inhibitory effect of micafungin on biofilm formation by Pseudomonas aeruginosa. Biofouling. 2013 Jul 23.2. Kai H, et al. Synergistic antifungal activity of KB425796-C in combination with micafungin against Aspergillus fumigat us and its eff