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Tebipenem

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Chemical Structure| 161715-21-5 同义名 : LJC 11036
CAS号 : 161715-21-5
货号 : A151161
分子式 : C16H21N3O4S2
纯度 : 98% (hydrate)
分子量 : 383.49
MDL号 : MFCD00936545
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(91.27 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 7 mg/mL(18.25 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 It is well known that carbapenem antibiotics have broad-spectrum activities and strong bactericidal actions against members of the family Enterobacteriaceae, Pseudomonas aeruginosa, and gram-positive cocci except methicillin-resistant Staphylococcus aureus and metallo-β-lactamase-producing pathogens. Tebipenem is a new oral carbapenem antibiotic. Tebipenem was very active against the S. pneumoniae isolates, with MICs of 0.002 to 0.031 μg/ml for the gPISP isolates and 0.016 to 0.125 μg/ml for the gPRSP isolates. The MICs of Tebipenem ranged from ≤0.001 to 0.004 μg/ml for all PSSP and gPISP (2x) isolates. S. pneumoniae isolates ME19 (serotype 19F) cell wall synthesis stopped in the pneumococcal cells exposed to Tebipenem at 0.063 μg/ml (the MIC) and 0.125 μg/ml (two times the MIC) for 2 h, and the protrusions were pulled in the direction of the long axis with the swelling of the cell[3]. In mouse, rat, dog and monkey, Tebipenem were absorbed quickly, and the bioavailability was 71.4, 59.1, 34.8 and 44.9%, respectively. After single oral administration of 10 mg/kg 14C-Tebipenem to rat, 36.9-42.7% and 58.3-62.2% of radioactivity was excreted to urine and feces, respectively, by 120 hours after administration[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.08mL

5.22mL

2.61mL
参考文献

[1]Hazra S, Xu H, Blanchard JS. Tebipenem, a new carbapenem antibiotic, is a slow substrate that inhibits the β-lactamase from Mycobacterium tuberculosis. Biochemistry. 2014 Jun 10;53(22):3671-8.

[2]Seenama C, Tiengrim S, Thamlikitkul V. In vitro activity of tebipenem against Burkholderia pseudomallei. Int J Antimicrob Agents. 2013 Oct;42(4):375.

[3]Kobayashi R, Konomi M, Hasegawa K, Morozumi M, Sunakawa K, Ubukata K. In vitro activity of tebipenem, a new oral carbapenem antibiotic, against penicillin-nonsusceptible Streptococcus pneumoniae. Antimicrob Agents Chemother. 2005;49(3):889‐894

[4] Kijima K, Morita J, Suzuki K, et al. Jpn J Antibiot. 2009;62(3):214‐240