ABT-492

用途用途应用生物活性靶点体内研究 ABT-492 试剂级价格

ABT-492

CAS号:189279-58-1
英文名:ABT-492
中文名:ABT-492
CBNumber:CB12561456
分子式:C18H12ClF3N4O4
分子量:440.76
MOL File:189279-58-1.mol

ABT-492化学性质

熔点 :238-241℃
沸点 :698.5±55.0 °C(Predicted)
密度 :1.796
储存条件 :2-8°C
溶解度 :DMSO (Slightly), Methanol (Very Slightly, Heated, Sonicated)
酸度系数(pKa) :5.49±0.50(Predicted)
形态 :powder
颜色 :white to beige
CAS 数据库 :189279-58-1

ABT-492性质、用途与生产工艺

用途
1-(6-氨基-3,5-二氟-2-吡啶基)-8-氯-6-氟-1,4-二氢-7-(3-羟基-1-氮杂环丁基)-4-氧代-3-喹啉羧酸是有效的抗肺炎链球菌和多种病原体的试剂和广谱阴离子氟喹诺酮。
用途
1-(6-氨基-3,5-二氟-2-吡啶基)-8-氯-6-氟-1,4-二氢-7-(3-羟基-1-氮杂环丁基)-4-氧代-3-喹啉羧酸是原料药德拉沙星的杂质，可用于实验室研发过程和化工医药合成过程中，德拉沙星是一种广谱氟喹诺酮类抗生素。德拉沙星具有广泛的活性，对耐药性的金黄色葡萄球菌，肺炎链球菌和肺炎克雷伯菌都有效。
应用
1-(6-氨基-3,5-二氟-2-吡啶基)-8-氯-6-氟-1,4-二氢-7-(3-羟基-1-氮杂环丁基)-4-氧代-3-喹啉羧酸是有机合成中间体和医药中间体，可用于实验室研发合成过程和化工生物研发过程中。
生物活性 Delafloxacin (ABT-492, RX-3341, WQ-3034)是一种氟喹诺酮，抗155需氧和171厌氧病原体。
靶点

Antibiotic

体内研究

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 log ₁₀ 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-log ₁₀ 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 (t _1/2 =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 (four S. aureus , four S. pneumoniae , and four K. 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 injection
Result:	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 mice
Dosage:	2.5, 10, 40, and 160 mg/kg; 0.2 mL
Administration:	Subcutaneous injection; 24 h
Result:	The maximum drug concentrations (C _max ) concentrations ranged from 2 to 71 mg/L. AUC _0-∞ 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 (t _1/2 ) ranged from 0.7 to 1 h.