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品質等級
化驗
≥93% (HPLC)
形狀
solid
製造商/商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
tan
溶解度
DMSO: 20 mg/mL
ethanol: 20 mg/mL
運輸包裝
wet ice
儲存溫度
−20°C
InChI
1S/C24H27NO7/c1-22(7-6-17(28)25-18-14(26)4-3-13(19(18)29)21(30)31)16(27)5-8-24-10-12-9-15(20(22)24)32-23(12,2)11-24/h3-5,8,12,15,20,26,29H,6-7,9-11H2,1-2H3,(H,25,28)(H,30,31)/t12-,15+,20+,22-,23+,24+/m1/s1
一般說明
A cell-permeable Streptomyces-derived antibiotic that exhibits broad-spectrum Gram-positive antibacterial activity by selectively targeting the elongation condensing enzyme FabF (IC50 = 48 and 160 nM against S. aureus and E. coli FabF, respectively), but not the initiation condensing enzyme FabH (IC50 = 67 µM), involved in type II fatty acid synthesis (FASII). Binding studies indicate that acyl-FabF intermediate complex formation induces a FabF conformation change that is necessary for Platensimycin interaction. Platensimycin effectively kills numerous Staphylococcus aureus, Enterococcus faecium, and Streptococcus pneumoniae strains, including the ones that are resistant to methicillin and vancomycin (Cat. No. 627850). Platensimycin does not exhibit antifungal activity towards Candida albicans (no effect at 64 µg/ml) or toxicity toward mammalian HeLa culture (no effect at 1000 µg/ml) and is efficacious in treating S. aureus infection in mice in vivo (~105-fold bacteria titre reduction via a 24 h i.v. at 150 µg h-1). Although Platensimycin is ineffective toward wild-type E. coli due to the presence of functional multidrug efflux pump (no effect at 64 µg/ml), Platensimycin does inhibit the growth of efflux-negative E. coli strains.
A cell-permeable Streptomyces-derived antibiotic that exhibits broad-spectrum Gram-positive antibacterial activity by selectively targeting the elongation condensing enzyme FabF (IC50 = 48 and 160 nM against S. aureus and E. coli FabF, respectively), but not the initiation condensing enzyme FabH (IC50 = 67 µM), involved in type II fatty acid synthesis (FASII). Binding studies indicate that acyl-FabF intermediate complex formation induces a FabF conformation change that is necessary for Platensimycin interaction. Platensimycin effectively kills numerous Staphylococcus aureus, Enterococcus faecium, and Streptococcus pneumoniae strains, including the ones that are resistant to methicillin and vancomycin (Cat. No. 627850). Platensimycin does not exhibit antifungal activity towards Candida albicans (no effect at 64 µg/ml) or toxicity toward mammalian HeLa culture (no effect at 1000 µg/ml) and is efficacious in treating S. aureus infection in mice in vivo (~105-fold bacteria titre reduction via a 24 h i.v. at 150 µg h-1). Although Platensimycin is ineffective toward wild-type E. coli due to the presence of functional multidrug efflux pump (no effect at 64 µg/ml), Platensimycin does inhibit the growth of efflux-negative E. coli strains. Platensimycin has been shown to potently and selectively inhibit hepatocyte FAS and fatty acid oxidation (FAO), without affecting sterol synthesis. Platensimycin is also known as Fatty Acid Synthase Inhibitor III.
警告
Toxicity: Harmful (C)
其他說明
Wu, M., et al. 2011. Proc. Natl. Acad. Sci. USAin press.
Wang, J., et al. 2007. Proc. Natl. Acad. Sci. USA104, 7612.
Singh, S.B., et al. 2006. J. Am. Chem. Soc.128, 11916.
Wang, J., et al. 2006. Nature441, 358.
Wang, J., et al. 2007. Proc. Natl. Acad. Sci. USA104, 7612.
Singh, S.B., et al. 2006. J. Am. Chem. Soc.128, 11916.
Wang, J., et al. 2006. Nature441, 358.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
分析證明 (COA)
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