产品
编 号:F581202
分子式:C73H112N22O16
分子量:1553.81
产品类型
结构图
CAS No: 944252-63-5
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产品详情
生物活性:
Murepavadin (POL7080), a 14-amino-acid cyclic peptide, is a highly potent, specific antibiotic. Murepavadin exhibits a potent antimicrobial activity for P. aeruginosa with both MIC50 and MIC90 values of 0.12 mg/L. Murepavadin also can target the lipopolysaccharide transport portin D. Murepavadin can be used for the research of bacterial resistance.
体内研究:
Murepavadin (s.c.; 0-100 mg/kg) is active in pre-clinical animal models including infections with XDR isolates.Animal Model:murine models of P. aeruginosa infection
Dosage:0-100 mg/kg
Administration:Subcutaneous, q24h or q12h
Result:Resulted in an increase in survival rate to 100% and showed significantly lower CFU levels both in the blood and in the peritoneal fluid at 2 and 10 mg/kg 1 h post-infection.
Animal Model:Mouse, rat, rabbit, and monkey
Dosage:0-5 mg/kg
Administration:Intraperitoneal or subcutaneous, single
Result:Followed a two-compartment model following intravenous administration and decline of plasma concentrations.Distributed into the aqueous phase of the body, and systemic plasma clearance (CL) values were similar to the species-specific glomerular filtration rates (GFRs) .Had high bioavailability (67.79%) after subcutaneous (s.c.) administration in rats but had low oral bioavailability (<0.01%).Had a linear relationship between ELF AUC and unbound plasma AUC in mouse.Did not readily cross the blood/brain barrier.
体外研究:
Murepavadin has activity against P. aeruginosa with MIC50 and MIC90 values both of 0.12 mg/L.Murepavadin inhibits megalin-mediated uptake of gentamicin in vitro with an IC50 value of 5.84 μM.