AFN-1252 (Synonyms: API-1252, Debio 1452) |
| カタログ番号GC40646 |
AFN-1252(Debio 1452) は、エノイル アシル キャリア タンパク質 レダクターゼ (FabI) の強力な阻害剤であり、0.12 μg/ml 以下の濃度で黄色ブドウ球菌および表皮ブドウ球菌のすべての臨床分離株を阻害しました。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 620175-39-5
Sample solution is provided at 25 µL, 10mM.
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AFN-1252(Debio 1452) is a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis at concentrations of ≤0.12 μg/ml. IC50 value:Target: Antibiotic agentAFN-1252 was inactive (MIC90, >4 μg/ml) against clinical isolates of Streptococcus pneumoniae, beta-hemolytic streptococci, Enterococcus spp., Enterobacteriaceae, nonfermentative gram-negative bacilli, and Moraxella catarrhalis. These data support the continued development of AFN-1252 for the treatment of patients with resistant staphylococcal infections.
References:
[1]. Karlowsky JA, et al. AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity. Antimicrob Agents Chemother. 2009 Aug;53(8):3544-8.
[2]. Narasimha Rao K, et al. AFN-1252 is a potent inhibitor of enoyl-ACP reductase from Burkholderia pseudomallei-Crystal structure, mode of action, and biological activity. Protein Sci. 2015 May;24(5):832-40.
[3]. Yao J, et al. Resistance to AFN-1252 arises from missense mutations in Staphylococcus aureus enoyl-acyl carrier protein reductase (FabI). J Biol Chem. 2013 Dec 20;288(51):36261-71.
[4]. Parsons JB, et al. Perturbation of Staphylococcus aureus gene expression by the enoyl-acyl carrier protein reductase inhibitor AFN-1252. Antimicrob Agents Chemother. 2013 May;57(5):2182-90.
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