Omadacycline tosylate  (Synonyms: 奥马环素; PTK 0796 tosylate; Amadacycline tosylate)

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^[1][2][3][4].

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^[2]。
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%^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

728.85

C₃₆H₄₈N₄O₁₀S

1075240-43-5

固体

White to yellow

奥马环素；奥玛环素甲磺酸盐；甲苯磺酸奥玛环素

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

• [1]. Durães F, et, al. Omadacycline: A Newly Approved Antibacterial from the Class of Tetracyclines. Pharmaceuticals (Basel). 2019 Apr 21;12(2):63.  [Content Brief]

  [2]. Macone AB, et, al. In vitro and in vivo antibacterial activities of omadacycline, a novel aminomethylcycline. Antimicrob Agents Chemother. 2014;58(2):1127-35.  [Content Brief]

  [3]. Zhanel GG, et, al. Omadacycline: A Novel Oral and Intravenous Aminomethylcycline Antibiotic Agent. Drugs. 2020 Feb;80(3):285-313.  [Content Brief]

  [4]. Markham A, et, al. Omadacycline: First Global Approval. Drugs. 2018 Dec;78(18):1931-1937.  [Content Brief]

  [5]. Tanaka SK, et al. In Vitro and In Vivo Assessments of Cardiovascular Effects with Omadacycline. Antimicrob Agents Chemother. 2016 Aug 22;60(9):5247-53.  [Content Brief]