Delafloxacin meglumine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

德拉沙星葡甲胺是一种广谱氟喹诺酮类抗生素。

Delafloxacin meglumine is a broad-spectrum fluoroquinolone antibiotic.(In Vivo):Delafloxacin (the total daily doses vary from 0.156 to 640 mg/kg/24 h, subcutaneous injection) is highly effective against S. aureus. Against all four strains are observed a decrease of 1.5 to 2.2 log10 CFU in organism burden from untreated controls at even the lowest dose studied, and for two strains (MW2 and R2527) there is net bactericidal activity at the lowest dose. At the maximal doses studied, there is a >4-log10 kill from initial burden for all S. aureus strains.Delafloxacin (2.5, 10, 40, and 160 mg/kg; subcutaneous injection, 24 h) has moderate terminal elimination half-life (t1/2=0.68 h, 0.79 h, 0.69 h and 1.0 h for 2.5 mg/kg, 10 mg/kg, 40 mg/kg, and 160 mg/kg, respectively).

——

Delafloxacin (the total daily doses vary from 0.156 to 640 mg/kg/24 h, subcutaneous injection) is highly effective against S. aureus. Against all four strains are observed a decrease of 1.5 to 2.2 log10 CFU in organism burden from untreated controls at even the lowest dose studied, and for two strains (MW2 and R2527) there is net bactericidal activity at the lowest dose. At the maximal doses studied, there is a >4-log10 kill from initial burden for all S. aureus strains.Delafloxacin (2.5, 10, 40, and 160 mg/kg; subcutaneous injection, 24 h) has moderate terminal elimination half-life (t1/2=0.68 h, 0.79 h, 0.69 h and 1.0 h for 2.5 mg/kg, 10 mg/kg, 40 mg/kg, and 160 mg/kg, respectively). Animal Model:Mice with a neutropenic murine lung infection model (fourS. aureus, four S. pneumoniae, and fourK. pneumoniae strains)Dosage:The total daily doses vary from 0.156 to 640 mg/kg/24 h Administration:0.03 to 160 mg/kg are administered every 6 h (q6h) to infected mice by subcutaneous injectionResult:Inhibited S. aureus strains ATCC 29213, ATCC 33591, MW2, R2527 with MICs of 0.008, 0.008, 0.004, and 0.004 mg/L, respectively.Inhibited S. pneumoniae strains ATCC 10813, ATCC 49619, 145, and 1329 with MICs of 0.03, 0.125, 0.016, and 0.016 mg/L, respectively.Inhibited K. pneumonia strains ATCC 43816, 4105, 4110, and 81-1260A with MICs of 0.06, 1, 0.5, and 0.06 mg/L, respectively.Animal Model:Neutropenic miceDosage:2.5, 10, 40, and 160 mg/kg; 0.2 mL Administration:Subcutaneous injection; 24 h Result:The maximum drug concentrations (Cmax) concentrations ranged from 2 to 71 mg/L. AUC0-∞ values ranged from 2.8 to 152 mg?h/L and were linear across the 2.5- to 160-mg dosing range. The elimination half-life (t1/2) ranged from 0.7 to 1 h.

ABT492 meglumine | RX-3341 meglumine | WQ-3034 meglumine

GPCR/G Protein

Antibacterial

Bacterial

——

Pneumonia

352458-37-8

635.97

C25H29ClF3N5O9

>98% (HPLC)

DMSO:6.4 mg/mL (10.06 mM);H2O:50 mg/mL (78.62 mM; Need ultrasonic)

CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.Nc1nc(c(F)cc1F)-n1cc(C(O)=O)c(=O)c2cc(F)c(N3CC(O)C3)c(Cl)c12

——

(-20℃)

With Ice Pack

≥ 2 years