Aztreonam 氨曲南
货号:
IA0060
品牌:
Jinpan
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产品简介
MDL | MFCD00072145 |
EC | EINECS 278-839-9 |
别名 | 菌克单 |
CAS | 78110-38-0 |
分子式 | C13H17N5O8S2 |
分子量 | 435.43 |
纯度 | HPLC≥98% |
单位 | 瓶 |
生物活性 | Aztreonam (also known as SQ 26776) is a synthetic monocyclic beta-lactam antibiotic, used to treat Gram-negative aerobic bacteria infection. It has a very high affinity for penicillin-binding protein 3 (PBP-3). Aztreonam causes significant suppression of human colony forming unit-erythroid (cfu-e), burst forming unit-erythroid (bfu-e) and colony forming unit-granulocyte macrophage (cfu-gm) at both peak and trough serum concentrations in human bone marrow cells. Aztreonam is hydrolyzed at measurable rates by class A beta-lactamases, a TEM-2 type penicillinase and the Proteus vulgaris cephalosporinase with a broad substraterange.[1-3] |
In Vitro | Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic (a monobactam), with the nucleus based on a simpler monobactam isolated from Chromobacterium violaceum. It was approved by the U.S. Food and Drug Administration in 1986. It is resistant to some beta-lactamases, but is inactivated by extended-spectrum beta-lactamases. Aztreonam has no useful activity against gram-positive or anaerobic microorganisms[1]. Aztreonam (SQ-26) is similar in action to penicillin. It inhibits mucopeptide synthesis in the bacterial cell wall, thereby blocking peptidogly can crosslinking. It has a very high affinity for penicillin-binding protein 3 (PBP-3) and mild affinity for PBP-1a. Aztreonam (SQ-26) binds the penicillin-binding proteins of gram-positive and anaerobic bacteria very poorly and is largely ineffective against them. Aztreonam (SQ-26) is bactericidal but less so than some of the cephalosporins[2]. |
In Vivo | Aztreonam (300 mg/kg) results in a significant decrease in the content of hepatic microsomal P450, while no significant change is observed in hepatic cytochrome b5 content and NADPH-cytochrome c (P450) reductase activity[3] |
SMILES | CC(C)(O/N=C(C1=CSC(N)=N1)C(N[C@H]2[C@H](C)N(S(=O)(O)=O)C2=O)=O)C(O)=O |
靶点 | Bacterial |
数据来源文献 | [1]. Kobayashi Y, et al. Synergy with aztreonam and arbekacin or tobramycin against Pseudomonas aeruginosa isolated from blood. J Antimicrob Chemother. 1992 Dec;30(6):871-2.
[2]. Guay DR, et al. Aztreonam, a new monobactam antimicrobial. Clin Pharm. 1985 Sep-Oct;4(5):516-26. |
规格 | 10mg 10mM*1mL (in DMSO) 50mg 100mg |
是单环β-内酰胺抗生素,与青霉素结合蛋白3(PBP-3)有较高亲和力。