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Purity: ≥98%
Omadacycline tosylate (formerly PTK0796; trade name: Nuzyra), the tosylate salt of omadacycline, is a tetracycline antibiotic being developed as an oral and intravenous (IV) formulation to treat community-acquired bacterial infections such as acute bacterial skin and skin structure infections (ABSSSI), community-acquired bacterial pneumonia (CABP), and urinary tract infections (UTI). In Oct 2018, Omadacycline was approved by FDA to treat community-acquired bacterial pneumonia and acute bacterial skin and skin structure infections.
| Targets |
Tetracycline
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| ln Vitro |
Omadacycline is a novel, aminomethyl tetracycline antibiotic being developed for oral and intravenous (IV) administration to treat community-acquired bacterial infections such as acute bacterial skin and skin structure infections (ABSSSI), community-acquired bacterial pneumonia (CABP), and urinary tract infections (UTI). In vitro, omadacycline has activity against Gram-positive and Gram-negative aerobes, anaerobes, and atypical pathogens including Legionella and Chlamydia spp. Omadacycline offers once daily oral and IV dosing and a clinical tolerability and safety profile that compares favorably with contemporary antibiotics used across serious community-acquired infections where resistance has rendered many less effective. In studies in patients with complicated skin and skin structure infections, including those with MRSA infections, omadacycline exhibited an efficacy and tolerability profile that was comparable to linezolid. Ongoing and planned clinical studies are evaluating omadacycline as monotherapy for treating serious community-acquired bacterial infections including Acute Bacterial Skin and Skin Structure Infections (ABSSSI) and Community-Acquired Bacterial Pneumonia (CABP). This review provides an overview of the discovery, microbiology, nonclinical data, and available clinical safety and efficacy data for omadacycline, with reference to other contemporary tetracycline-derived antibiotics.
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| Cell Assay |
Omadacycline MIC90s for MRSA, VRE, and beta-hemolytic streptococci are 1.0 μg/mL, 0.25 μg/mL, and 0.5 μg/mL, correspondingly. For PRSP and H. influenzae, the corresponding omadacycline MIC90s are 0.25 μg/ml and 2.0 μg/mL. Omadacycline exhibits efficacy against organisms that exhibit both ribosomal protection and active tetracycline efflux, the two main mechanisms of resistance[1]. Omadacycline has little effect on the synthesis of DNA, RNA, or peptidoglycans, but it inhibits the synthesis of proteins. Furthermore, omadacycline exhibits enhanced binding, comparable to tigecycline, to the tetracycline binding site on the 30S subunit of the bacterial ribosome due to additional molecular interactions.
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| References |
| Molecular Formula |
C36H48N4O10S
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|---|---|
| Molecular Weight |
728.86
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| Exact Mass |
728.31
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| Elemental Analysis |
C, 59.33; H, 6.64; N, 7.69; O, 21.95; S, 4.40
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| CAS # |
1075240-43-5
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| Related CAS # |
Omadacycline;389139-89-3;Omadacycline hydrochloride;1196800-39-1;Omadacycline-d9;2272886-41-4;Omadacycline mesylate;1196800-40-4
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| Appearance |
Solid powder
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| SMILES |
O=C(C1=C(O)[C@@H](N(C)C)[C@@](C[C@@]2([H])C(C(C3=C(O)C(CNCC(C)(C)C)=CC(N(C)C)=C3C2)=O)=C4O)([H])[C@@]4(O)C1=O)N.O=S(C5=CC=C(C)C=C5)(O)=O
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| InChi Key |
SETFNHZTVGTBHC-XGLFQKEBSA-N
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| InChi Code |
InChI=1S/C29H40N4O7.C7H8O3S/c1-28(2,3)12-31-11-14-10-17(32(4)5)15-8-13-9-16-21(33(6)7)24(36)20(27(30)39)26(38)29(16,40)25(37)18(13)23(35)19(15)22(14)34;1-6-2-4-7(5-3-6)11(8,9)10/h10,13,16,21,31,34,36-37,40H,8-9,11-12H2,1-7H3,(H2,30,39);2-5H,1H3,(H,8,9,10)/t13-,16-,21-,29-;/m0./s1
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| Chemical Name |
(4S,4aS,5aR,12aS)-4,7-bis(dimethylamino)-3,10,12,12a-tetrahydroxy-9-((neopentylamino)methyl)-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide 4-methylbenzenesulfonate
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| Synonyms |
PTK 0796 tosylate; PTK-0796; PTK0796; Amadacyclintosylate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 12.5 100 mg/mL ( 137.2 mM )
Water : 100 mg/mL Ethanol : 100 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (68.60 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3720 mL | 6.8600 mL | 13.7201 mL | |
| 5 mM | 0.2744 mL | 1.3720 mL | 2.7440 mL | |
| 10 mM | 0.1372 mL | 0.6860 mL | 1.3720 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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