产品
编 号:F028449
分子式:C36H48N4O10S
分子量:728.85
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1mg
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5mg
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10mg
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25mg
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生物活性:
Omadacycline (PTK 0796) tosylate, a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline tosylate acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline tosylate possesses broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria. Omadacycline tosylate can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections.

体内研究:
Omadacycline (0.11-18 mg/kg;单次静脉注射) 对小鼠全身感染中的肺炎链球菌、大肠杆菌和金黄色葡萄球菌具有功效模型,ED50 范围为 0.30 mg/kg 至 3.39 mg/kg。

体外研究:
Omadacycline 对耐甲氧西林金黄色葡萄球菌 (MRSA)、耐万古霉素肠球菌 (VRE)、β-溶血性链球菌、耐青霉素肺炎链球菌 (PRSP) 和流感嗜血杆菌 (H.influenzae) 具有活性,MIC90 分别为 1.0、0.25、0.5、0.25 和 2.0 μg/mL[ 2]。Omadacycline 通过核糖体保护和活性四环素外排对表达四环素和其他抗生素耐药性的菌株具有活性。Omadacycline (10 μM) 可抑制毒蕈碱乙酰胆碱受体 (M2) 的配体结合活性达 82%。
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