AFN-1252
Based on 12 publication(s) in Google Scholar
AFN-1252 is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 exhibits typical MIC90 values of ⩽0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith.
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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: 99.49%
- CAS 番号: 620175-39-5
- 分子式: C22H21N3O3
- 分子量:375.42
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 AFN-1252
More- Nat Commun. 2016 Oct 5;7:12944. [Abstract]
- Phytomedicine.2024 May 13:130:155732. [Abstract]
- Cell Rep. 2019 Dec 17;29(12):3974-3982.e4. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- J Lipid Res. 2024 Nov 4:100693. [Abstract]
- PLoS Pathog. 2020 Oct 30;16(10):e1008529. [Abstract]
- Antimicrob Agents Chemother. 2019 Mar 27;63(4):e02105-18. [Abstract]
- PLoS Genet. 2026 May 27;22(5):e1012165. [Abstract]
- Patent. US20250270197A1.
- University of Washington. 2024.
- bioRxiv. 2023 Jun 30:2023.06.29.547085. [Abstract]
- Patent. US20210017165A1.
Antibiotic アイソフォーム固有の製品をすべて表示
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生物活性
AFN-1252 is extremely potent against clinical isolates of S. aureus (MIC90, 0.015 μg/ml) and coagulase-negative staphylococci (MIC90, 0.12 μg/ml)[2]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female 5- to 6-week-old CD-1 mice (18 to 22 g) with S. aureus Smith bacterial inoculum[2]
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Dosage:0.03, 0.1, 0.3, 1, 3 mg/kg
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Administration:Oral gavage; single dose
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Result:Was efficacious in a mouse model of septicemia, with 100% survival obtained with a single oral dose of 1 mg/kg.
The calculated ED50s (95% confidence limits) were 0.15 (0.11 to 0.21) mg/kg.
化学情報
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CAS 番号 620175-39-5
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性状 Solid
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分子量 375.42
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分子式 C22H21N3O3
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Color White to off-white
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SMILES
O=C(N(C)CC1=C(C)C2=CC=CC=C2O1)/C=C/C(C=C3CC4)=CNC3=NC4=O
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別名
API-1252; Debio 1452
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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 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Nat Commun
Environmental fatty acids enable emergence of infectious Staphylococcus aureus resistant to FASII-targeted antimicrobials. [Abstract]2016 Oct 5;7:12944. PMID: 27703138 -
Phytomedicine
In vitro and in vivo enhancement effect of glabridin on the antibacterial activity of colistin, against multidrug resistant Escherichia coli strains. [Abstract]2024 May 13:130:155732. PMID: 38776738 -
Cell Rep
Permissive Fatty Acid Incorporation Promotes Staphylococcal Adaptation to FASII Antibiotics in Host Environments. [Abstract]2019 Dec 17;29(12):3974-3982.e4. PMID: 31851927 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
J Lipid Res
2024 Nov 4:100693. PMID: 39505263 -
PLoS Pathog
Triclosan depletes the membrane potential in Pseudomonas aeruginosa biofilms inhibiting aminoglycoside induced adaptive resistance. [Abstract]2020 Oct 30;16(10):e1008529. PMID: 33125434 -
Antimicrob Agents Chemother
A FASII Inhibitor Prevents Staphylococcal Evasion of Daptomycin by Inhibiting Phospholipid Decoy Production. [Abstract]2019 Mar 27;63(4):e02105-18. PMID: 30718253 -
PLoS Genet
FabF and FadM cooperate to recycle fatty acids and rescue ∆plsX lethality in Staphylococcus aureus. [Abstract]2026 May 27;22(5):e1012165. PMID: 42201948 -
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bioRxiv
Elucidating the Impact of Bacterial Lipases, Human Serum Albumin, and FASII Inhibition on the Utilization of Exogenous Fatty Acids by Staphylococcus aureus. [Abstract]2023 Jun 30:2023.06.29.547085. PMID: 37425828 -
溶剤 & 溶解度
DMSO : 5.8 mg/mL (15.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (272 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Nachum Kaplan, et al. In vitro activity (MICs and rate of kill) of AFN-1252, a novel FabI inhibitor, in the presence of serum and in combination with other antibiotics. J Chemother. 2013 Feb;25(1):18-25. [Content Brief]
[2]. Nachum Kaplan,et al. Mode of action, in vitro activity, and in vivo efficacy of AFN-1252, a selective antistaphylococcal FabI inhibitor. Antimicrob Agents Chemother. 2012 Nov;56(11):5865-74. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6637 mL | 13.3184 mL | 26.6368 mL | 66.5921 mL |
| 5 mM | 0.5327 mL | 2.6637 mL | 5.3274 mL | 13.3184 mL | |
| 10 mM | 0.2664 mL | 1.3318 mL | 2.6637 mL | 6.6592 mL | |
| 15 mM | 0.1776 mL | 0.8879 mL | 1.7758 mL | 4.4395 mL |
AFN-1252 関連分類
HY-16911 関連分類
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