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Omadacycline tosylate

MCE China：Omadacycline tosylate

Brand：MedChemExpress (MCE)

Cat. No.HY-14865B

CAS：1075240-43-5

Synonyms：PTK 0796 tosylate; Amadacycline tosylate

Purity：99.37%

Storage：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)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：Omadacycline displays activity against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE), beta-hemolytic streptococci, penicillin-resistant Streptococcus pneumonia (PRSP) and Haemophilus influenzae (H. influenzae), with MIC90s of 1.0, 0.25, 0.5, 0.25 and 2.0 μg/mL respectively[2]. Omadacycline is active against strains expressing tetracycline and other antibiotics resistance by ribosomal protection and active tetracycline efflux[2]. Omadacycline (10 μM) inhibits the ligand binding activity of muscarinic acetylcholine receptor (M2) by 82%[5].

In Vivo：Omadacycline (0.11-18 mg/kg; a single i.v.) exhibits efficacy against Streptococcus pneumonia, Escherichia coli, and Staphylococcus aureus in mice systemic infection model, with ED50s ranging from 0.30 mg/kg to 3.39 mg/kg[2].

IC50 & Target：Tetracycline

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References：

[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]