Biapenem

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Chemical Structure| 120410-24-4 同义名 : CLI 86815;L 627;Omegacin;RPX2003;CL 186815;LJC 10627
CAS号 : 120410-24-4
货号 : A699164
分子式 : C15H18N4O4S
纯度 : 98%
分子量 : 350.393
MDL号 : MFCD00864863
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 10 mg/mL(28.54 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Biapenem is a new parenteral carbapenem antibacterial agent with a broad spectrum of in vitro antibacterial activity encompassing many Gram-negative and Gram-positive aerobic and anaerobic bacteria, including species producing beta-lactamases[3]. The bicyclic derivative of biapenem has significant affinity for B2 MβLs (B2 metallo β-lactamases), and that it may be possible to obtain clinically effective inhibitors of these enzymes by modification of this lead compound[4]. Biapenem showed good clinical and bacteriological efficacy (similar to that of imipenem/cilastatin) in the treatment of adult patients with intra-abdominal infections, lower respiratory infections or complicated urinary tract infections[3]. Biapenem is effective and safe for treating FN (febrile neutropenia)[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01702649 Healthy Volunteers ... 展开 >> Bacterial Infections 收起 << Phase 1 Completed - United States, Arizona ... 展开 >> Celerion Tempe, Arizona, United States, 85283 收起 <<
NCT01772836 Healthy Volunteers ... 展开 >> Bacterial Infections 收起 << Phase 1 Completed - Australia, South Australia ... 展开 >> CMAX Adelaide, South Australia, Australia, 5000 收起 <<
NCT01751269 Healthy Volunteers ... 展开 >> Bacterial Infections 收起 << Phase 1 Completed - Australia, South Australia ... 展开 >> CMAX Adelaide, South Australia, Australia, 5000 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.27mL

2.85mL

1.43mL

28.54mL

5.71mL

2.85mL
参考文献

[1]Perry CM, Ibbotson T. Biapenem. Drugs. 2002;62(15):2221-34; discussion 2235.

[2]Aldridge KE, Morice N, Schiro DD. In vitro activity of biapenem (L-627), a new carbapenem, against anaerobes. Antimicrob Agents Chemother. 1994 Apr;38(4):889-93.

[3]Perry CM, Ibbotson T. Biapenem. Drugs. 2002;62(15):2221-34; discussion 2235.

[4]Gatti DL. Biapenem inactivation by B2 metallo β-lactamases: energy landscape of the post-hydrolysis reactions. PLoS One. 2012;7(1):e30079.

[5]Kasahara S, Hara T, Tsurumi H, Goto N, Kanemura N, Yoshikawa T, Yamada T, Sawada M, Takahashi T, Moriwaki H. [Clinical effects of biapenem on febrile neutropenia in patients with hematological malignancy]. Jpn J Antibiot. 2008 Jun;61(3):115-21.