Apramycin
Based on 5 publication(s) in Google Scholar
Apramycin (Nebramycin II) is an orally active, acidic pH tolerant and aminoglycoside-modifying-enzymes-tolerant aminoglycoside antibiotic which inhibits protein biosynthesis by targeting the bacterial ribosome. Apramycin is a potential anti-drug-resistance antibiotic.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.80%
- CAS 番号: 37321-09-8
- 分子式: C21H41N5O11
- 分子量:539.58
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 Apramycin
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生物活性
Apramycin (4 mg/L) inhibits 99% of K. pneumoniae and 93% of Enterobacter clinical isolates. Apramycin (8 mg/L) inhibits 99% of all E. coli, 98% of C. freundii, 96% of Providencia spp., 92% of S. marcescens, 97% of M. morganii and 100% of P. mirabilis clinical isolates, exhibiting significantly better antimicrobial activity than the clinical standard-of-care aminoglycosides Gentamicin and Amikacin[1].
Apramycin (100 μM, 10 min) exerts an 11% decrease in cytoplasmic uptake of E.coli when lowering the pH from 7.3 to 5.7 while the amounts of Gentamicin and Amikacin are reduced by 62% and 51%, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Apramycin (16, 32, 80 mg/kg, s.c., 24 h) dose-dependently reduces bacterial burden in the kidneys between 2-5 log10 and in blood between 2-3 log10 for neutropenic model of Staphylococcus aureus septicemia mice[2].
Apramycin (50 mg/kg/d, s.c., 21 d) induces nephrotoxicity scores comparable to those induced by Gentamicin (10 mg/kg/d)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:M. tuberculosis low-dose aerosol infection model of IFN-γ knockout mice [2]
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Dosage:200 mg/kg/d
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Administration:Subcutaneousinjection (s.c.) for 9 d
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Result:Showed a 2.4-log10 CFU reduction and better antituberculous activity compared to Amikacin (1.8-log10 reduction).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 37321-09-8
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性状 Solid
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分子量 539.58
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分子式 C21H41N5O11
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Color White to light yellow
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SMILES
O[C@H]1[C@](O[C@H](O[C@@]([C@H](C[C@H]2N)N)([H])[C@@H]([C@H]2O)O)[C@H](N)C3)([H])[C@@]3([H])O[C@H](O[C@@]([C@@H]([C@@H](O)[C@@H]4N)O)([H])O[C@@H]4CO)[C@H]1NC
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別名
Nebramycin II
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Microbiol
Prodrug florfenicol amine is activated by intrinsic resistance to target Mycobacterium abscessus. [Abstract]2025 Nov;10(11):2875-2891. PMID: 41168430 -
Nat Microbiol
Characterization of antibiotic resistomes by reprogrammed bacteriophage-enabled functional metagenomics in clinical strains. [Abstract]2023 Mar;8(3):410-423. PMID: 36759752 -
J Adv Res
WTAP/YTHDF1-mediated m6A modification amplifies IFN-γ-induced immunosuppressive properties of human MSCs. [Abstract]2024 Jun 27:S2090-1232(24)00256-X. PMID: 38944238 -
Nucleic Acids Res
PhoP-regulated VirK acts as an accessory factor to maintain virulence in polymyxin-resistant Klebsiella pneumoniae. [Abstract]2026 Apr 23;54(8):gkag290. PMID: 42033226 -
Acta Pharm Sin B
Polymyxin resistance caused by large-scale genomic inversion due to IS 26 intramolecular translocation in Klebsiella pneumoniae. [Abstract]2023 Sep;13(9):3678-3693. PMID: 37719365
溶剤 & 溶解度
H2O : ≥ 50 mg/mL (92.66 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (280 KB)
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SDS (537 KB)
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- Français - FR (537 KB)
- Deutsch - DE (537 KB)
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- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Juhas M, et al. In vitro activity of apramycin against multidrug-, carbapenem- and aminoglycoside-resistant Enterobacteriaceae and Acinetobacter baumannii. J Antimicrob Chemother. 2019;74(4):944-952. [Content Brief]
[2]. Meyer M, et al. In vivo efficacy of apramycin in murine infection models. Antimicrob Agents Chemother. 2014 Nov;58(11):6938-41. [Content Brief]
[3]. Becker K, et al. Antibacterial activity of apramycin at acidic pH warrants wide therapeutic window in the treatment of complicated urinary tract infections and acute pyelonephritis. EBioMedicine. 2021 Nov;73:103652. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.8533 mL | 9.2665 mL | 18.5329 mL | 46.3323 mL |
| 5 mM | 0.3707 mL | 1.8533 mL | 3.7066 mL | 9.2665 mL | |
| 10 mM | 0.1853 mL | 0.9266 mL | 1.8533 mL | 4.6332 mL | |
| 15 mM | 0.1236 mL | 0.6178 mL | 1.2355 mL | 3.0888 mL | |
| 20 mM | 0.0927 mL | 0.4633 mL | 0.9266 mL | 2.3166 mL | |
| 25 mM | 0.0741 mL | 0.3707 mL | 0.7413 mL | 1.8533 mL | |
| 30 mM | 0.0618 mL | 0.3089 mL | 0.6178 mL | 1.5444 mL | |
| 40 mM | 0.0463 mL | 0.2317 mL | 0.4633 mL | 1.1583 mL | |
| 50 mM | 0.0371 mL | 0.1853 mL | 0.3707 mL | 0.9266 mL | |
| 60 mM | 0.0309 mL | 0.1544 mL | 0.3089 mL | 0.7722 mL | |
| 80 mM | 0.0232 mL | 0.1158 mL | 0.2317 mL | 0.5792 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.