AFN-1252 (Synonyms: API-1252, Debio 1452) |
| رقم الكتالوجGC40646 |
AFN-1252 (Debio 1452) هو مثبط قوي لانزيم اختزال البروتين الحامل لإنويل أسيل (FabI) ==، وهو يثبط جميع العزلات السريرية للمكورات العنقودية الذهبية والمكورات العنقودية البشروية بتركيزات ≤0.12 ميكروغرام / مل
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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