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编 号:F715428
分子式:C52H82ClN15O12
分子量:1144.75
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生物活性:
Upleganan (SPR206), a polymyxin analogue, and shows antibiotic activity against multidrug resistant Gram-negative pathogen. The MIC values of Upleganan against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301 are both 0.125 mg/L.

体内研究:
Upleganan (SPR206) (0.125-30 mg/kg; intravenous injection or subcutaneous injection; every 8 hours or every 4 hours; for 16 hours or 24 hours; neutropenic mice) treatment reduces the burden of Pa14 and NCTC13301 in lung tissue and in the thigh model.Animal Model:Neutropenic mice infected Pa14 or NCTC13301
Dosage:3 mg/kg, 10 mg/kg, 20 mg/kg, 30 mg/kg (intravenous injection); 0.125 mg/kg, 0.5 mg/kg, 1 mg/kg, 4 mg/kg (subcutaneous injection)
Administration:Intravenous injection or subcutaneous injection; every 8 hours or every 4 hours; for 16 hours or 24 hours
Result:In lung tissue, reduced the burden of Pa14 and NCTC13301 by 1.5 and 3.6 log10 CFU/mL. In the thigh model, reduced the burden of Ab13301 by 3.4 and 4.3 log10 CFU/g.

体外研究:
Upleganan (SPR206) exhibits strong anti-microbial properties against Gram-negative bacteria. The MIC values of SPR206 against E. coli IHMA558090, E. coli ATCC 25922, K. pneumonia ATCC 13882, P. aeruginosa ATCC 27853, A. baumannii NCTC13424 and A. baumannii ATCC 19003 are 8 mg/L, 0.125 mg/L, 0.125 mg/L, 0.25 mg/L, 0.06 mg/L and 0.125 mg/L, respectively, together with lower cytotoxicity .
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